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PD-0332991 (Palbociclib) Isethionate CDK4/6 inhibitor
N. Cat.: S1579
Struttura chimica
Peso molecolare: 573.66
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Controllo Qualità (Quality Control)
Lotto:
Purezza:
99.99%
99.99
Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)
| Linee cellulari | Tipo di saggio | Concentrazione | Tempo di incubazione | Formulazione | Descrizione dell'attività | PMID |
|---|---|---|---|---|---|---|
| H157 | Growth Inhibition Assay | 0-100 μM | 72 h | IC50=9 μM | 26390342 | |
| H2170 | Growth Inhibition Assay | 0-100 μM | 72 h | IC50=5 μM | 26390342 | |
| H520 | Growth Inhibition Assay | 0-100 μM | 72 h | IC50=0.73 μM | 26390342 | |
| H596 | Growth Inhibition Assay | 0-100 μM | 72 h | IC50=12 μM | 26390342 | |
| IMR-32 | Growth Inhibition Assay | 48 h | DMSO | IC50=261 nM | 26225123 | |
| SH-SY5Y | Growth Inhibition Assay | 48 h | DMSO | IC50=676 nM | 26225123 | |
| NGP | Growth Inhibition Assay | 48 h | DMSO | IC50=2.077 μM | 26225123 | |
| SH-EP | Growth Inhibition Assay | 48 h | DMSO | IC50=2.211 μM | 26225123 | |
| IMR-32 | Growth Inhibition Assay | 1 μM | 24 h | DMSO | induces G1 arrest | 26225123 |
| SH-SY5Y | Growth Inhibition Assay | 1 μM | 24 h | DMSO | induces G1 arrest | 26225123 |
| NGP | Growth Inhibition Assay | 1 μM | 24 h | DMSO | induces G1 arrest | 26225123 |
| SH-EP | Growth Inhibition Assay | 1 μM | 24 h | DMSO | induces G1 arrest | 26225123 |
| NGP | Fuction Assay | 0-1 μM | 24 h | DMSO | reduces the expression of TOP2A, CCNE2, and TK1 in a dose-dependent manner | 26225123 |
| IMR-32 | Fuction Assay | 0-1 μM | 24 h | DMSO | reduces the expression of TOP2A, CCNE2, and TK1 in a dose-dependent manner | 26225123 |
| U-CH2 | Growth Inhibition Assay | 0-1 μM | 72 h | IC50=50.2 nM | 26183925 | |
| U-CH3 | Growth Inhibition Assay | 0-1 μM | 72 h | IC50=52 nM | 26183925 | |
| U-CH6 | Growth Inhibition Assay | 0-1 μM | 72 h | IC50=90 nM | 26183925 | |
| U-CH7 | Growth Inhibition Assay | 0-1 μM | 72 h | IC50=98 nM | 26183925 | |
| U-CH11 | Growth Inhibition Assay | 0-1 μM | 72 h | IC50=340 nM | 26183925 | |
| MCF7 | Fuction Assay | 2.5-250 nM | 24 h | reduces Rb phosphorylation | 25991817 | |
| MV4-11 | Apoptosis Assay | 0.5 μM | 24 h | enhances apoptosis induced by sorafenib and AC220 | 25487917 | |
| MOLM13 | Apoptosis Assay | 0.5 μM | 24 h | enhances apoptosis induced by sorafenib and AC220 | 25487917 | |
| MOLM13-ITD alone | Growth Inhibition Assay | IC50=0.089 ± 0.009 μM | 25487917 | |||
| MV4-11-ITD alone | Growth Inhibition Assay | IC50=0.092 ± 0.008 μM | 25487917 | |||
| MOLM13-ITD/D835Y | Growth Inhibition Assay | IC50=0.114 ± 0.011 μM | 25487917 | |||
| MV4-11-ITD/D835V | Growth Inhibition Assay | IC50=0.116 ± 0.011 μM | 25487917 | |||
| MV4-11-ITD/D835V | Growth Inhibition Assay | IC50=0.102 ± 0.006 μM | 25487917 | |||
| MV4-11-ITD/F691L | Growth Inhibition Assay | IC50=0.112 ± 0.015 μM | 25487917 | |||
| MV4-11-ITD/N841K | Growth Inhibition Assay | IC50=0.113 ± 0.002 μM | 25487917 | |||
| U937-FLT3 WT | Growth Inhibition Assay | IC50=0.102 ± 0.013 μM | 25487917 | |||
| P12-ICHIKAWA | Growth Inhibition assay | IC50 = 0.09604 μM | SANGER | |||
| 697 | Growth Inhibition assay | IC50 = 0.14838 μM | SANGER | |||
| NB69 | Growth Inhibition assay | IC50 = 0.1618 μM | SANGER | |||
| EoL-1-cell | Growth Inhibition assay | IC50 = 0.18726 μM | SANGER | |||
| BHT-101 | Growth Inhibition assay | IC50 = 0.19825 μM | SANGER | |||
| SK-NEP-1 | Growth Inhibition assay | IC50 = 0.22002 μM | SANGER | |||
| MHH-NB-11 | Growth Inhibition assay | IC50 = 0.22019 μM | SANGER | |||
| AsPC-1 | Growth Inhibition assay | IC50 = 0.25253 μM | SANGER | |||
| ES1 | Growth Inhibition assay | IC50 = 0.25625 μM | SANGER | |||
| LAMA-84 | Growth Inhibition assay | IC50 = 0.25819 μM | SANGER | |||
| MOLT-16 | Growth Inhibition assay | IC50 = 0.25849 μM | SANGER | |||
| ES7 | Growth Inhibition assay | IC50 = 0.27309 μM | SANGER | |||
| KY821 | Growth Inhibition assay | IC50 = 0.3141 μM | SANGER | |||
| RT-112 | Growth Inhibition assay | IC50 = 0.32105 μM | SANGER | |||
| HL-60 | Growth Inhibition assay | IC50 = 0.34066 μM | SANGER | |||
| MOLT-4 | Growth Inhibition assay | IC50 = 0.34513 μM | SANGER | |||
| KARPAS-45 | Growth Inhibition assay | IC50 = 0.37616 μM | SANGER | |||
| SK-N-AS | Growth Inhibition assay | IC50 = 0.38783 μM | SANGER | |||
| CTB-1 | Growth Inhibition assay | IC50 = 0.40502 μM | SANGER | |||
| NKM-1 | Growth Inhibition assay | IC50 = 0.41189 μM | SANGER | |||
| HTC-C3 | Growth Inhibition assay | IC50 = 0.43295 μM | SANGER | |||
| BE-13 | Growth Inhibition assay | IC50 = 0.44427 μM | SANGER | |||
| KOSC-2 | Growth Inhibition assay | IC50 = 0.4669 μM | SANGER | |||
| NB14 | Growth Inhibition assay | IC50 = 0.48358 μM | SANGER | |||
| CAL-27 | Growth Inhibition assay | IC50 = 0.49459 μM | SANGER | |||
| H9 | Growth Inhibition assay | IC50 = 0.49543 μM | SANGER | |||
| RS4-11 | Growth Inhibition assay | IC50 = 0.50473 μM | SANGER | |||
| PA-1 | Growth Inhibition assay | IC50 = 0.50986 μM | SANGER | |||
| MV-4-11 | Growth Inhibition assay | IC50 = 0.51385 μM | SANGER | |||
| OS-RC-2 | Growth Inhibition assay | IC50 = 0.52162 μM | SANGER | |||
| RPMI-8226 | Growth Inhibition assay | IC50 = 0.52686 μM | SANGER | |||
| HGC-27 | Growth Inhibition assay | IC50 = 0.56499 μM | SANGER | |||
| CHP-212 | Growth Inhibition assay | IC50 = 0.59359 μM | SANGER | |||
| NB10 | Growth Inhibition assay | IC50 = 0.59918 μM | SANGER | |||
| HH | Growth Inhibition assay | IC50 = 0.59943 μM | SANGER | |||
| EW-16 | Growth Inhibition assay | IC50 = 0.60352 μM | SANGER | |||
| ES8 | Growth Inhibition assay | IC50 = 0.60521 μM | SANGER | |||
| HAL-01 | Growth Inhibition assay | IC50 = 0.60567 μM | SANGER | |||
| A204 | Growth Inhibition assay | IC50 = 0.63391 μM | SANGER | |||
| MHH-PREB-1 | Growth Inhibition assay | IC50 = 0.63699 μM | SANGER | |||
| EM-2 | Growth Inhibition assay | IC50 = 0.65064 μM | SANGER | |||
| BV-173 | Growth Inhibition assay | IC50 = 0.65248 μM | SANGER | |||
| ONS-76 | Growth Inhibition assay | IC50 = 0.67782 μM | SANGER | |||
| KM-H2 | Growth Inhibition assay | IC50 = 0.69554 μM | SANGER | |||
| D-263MG | Growth Inhibition assay | IC50 = 0.71712 μM | SANGER | |||
| ES3 | Growth Inhibition assay | IC50 = 0.72893 μM | SANGER | |||
| VA-ES-BJ | Growth Inhibition assay | IC50 = 0.73227 μM | SANGER | |||
| NBsusSR | Growth Inhibition assay | IC50 = 0.74299 μM | SANGER | |||
| NCI-H520 | Growth Inhibition assay | IC50 = 0.74652 μM | SANGER | |||
| ES5 | Growth Inhibition assay | IC50 = 0.7528 μM | SANGER | |||
| T-24 | Growth Inhibition assay | IC50 = 0.77871 μM | SANGER | |||
| SW962 | Growth Inhibition assay | IC50 = 0.80863 μM | SANGER | |||
| EW-3 | Growth Inhibition assay | IC50 = 0.80876 μM | SANGER | |||
| RXF393 | Growth Inhibition assay | IC50 = 0.81279 μM | SANGER | |||
| U251 | Growth Inhibition assay | IC50 = 0.81388 μM | SANGER | |||
| CAMA-1 | Growth Inhibition assay | IC50 = 0.83394 μM | SANGER | |||
| JVM-3 | Growth Inhibition assay | IC50 = 0.85178 μM | SANGER | |||
| COLO-800 | Growth Inhibition assay | IC50 = 0.89778 μM | SANGER | |||
| OVCAR-5 | Growth Inhibition assay | IC50 = 0.9001 μM | SANGER | |||
| LB1047-RCC | Growth Inhibition assay | IC50 = 0.92756 μM | SANGER | |||
| SW954 | Growth Inhibition assay | IC50 = 0.92941 μM | SANGER | |||
| J-RT3-T3-5 | Growth Inhibition assay | IC50 = 0.93606 μM | SANGER | |||
| Mewo | Growth Inhibition assay | IC50 = 0.9366 μM | SANGER | |||
| NCI-H1770 | Growth Inhibition assay | IC50 = 0.94055 μM | SANGER | |||
| HO-1-N-1 | Growth Inhibition assay | IC50 = 0.96281 μM | SANGER | |||
| HSC-3 | Growth Inhibition assay | IC50 = 0.96648 μM | SANGER | |||
| TYK-nu | Growth Inhibition assay | IC50 = 0.99825 μM | SANGER | |||
| KYSE-150 | Growth Inhibition assay | IC50 = 1.00076 μM | SANGER | |||
| SN12C | Growth Inhibition assay | IC50 = 1.00875 μM | SANGER | |||
| MOLT-13 | Growth Inhibition assay | IC50 = 1.01421 μM | SANGER | |||
| TE-11 | Growth Inhibition assay | IC50 = 1.04812 μM | SANGER | |||
| DB | Growth Inhibition assay | IC50 = 1.07273 μM | SANGER | |||
| CAL-39 | Growth Inhibition assay | IC50 = 1.07522 μM | SANGER | |||
| A3-KAW | Growth Inhibition assay | IC50 = 1.08408 μM | SANGER | |||
| CHP-134 | Growth Inhibition assay | IC50 = 1.11807 μM | SANGER | |||
| TGW | Growth Inhibition assay | IC50 = 1.12395 μM | SANGER | |||
| QIMR-WIL | Growth Inhibition assay | IC50 = 1.13134 μM | SANGER | |||
| NCI-SNU-1 | Growth Inhibition assay | IC50 = 1.16354 μM | SANGER | |||
| CGTH-W-1 | Growth Inhibition assay | IC50 = 1.17186 μM | SANGER | |||
| MHH-ES-1 | Growth Inhibition assay | IC50 = 1.17986 μM | SANGER | |||
| LB2241-RCC | Growth Inhibition assay | IC50 = 1.1862 μM | SANGER | |||
| ML-2 | Growth Inhibition assay | IC50 = 1.20734 μM | SANGER | |||
| COR-L23 | Growth Inhibition assay | IC50 = 1.22933 μM | SANGER | |||
| BFTC-905 | Growth Inhibition assay | IC50 = 1.24267 μM | SANGER | |||
| Hs-578-T | Growth Inhibition assay | IC50 = 1.25817 μM | SANGER | |||
| KG-1 | Growth Inhibition assay | IC50 = 1.26686 μM | SANGER | |||
| HEL | Growth Inhibition assay | IC50 = 1.29338 μM | SANGER | |||
| A549 | Growth Inhibition assay | IC50 = 1.29399 μM | SANGER | |||
| COLO-741 | Growth Inhibition assay | IC50 = 1.32089 μM | SANGER | |||
| PC-3 | Growth Inhibition assay | IC50 = 1.35221 μM | SANGER | |||
| HOS | Growth Inhibition assay | IC50 = 1.35296 μM | SANGER | |||
| HT-1080 | Growth Inhibition assay | IC50 = 1.37519 μM | SANGER | |||
| TE-8 | Growth Inhibition assay | IC50 = 1.41774 μM | SANGER | |||
| BHY | Growth Inhibition assay | IC50 = 1.46923 μM | SANGER | |||
| BB65-RCC | Growth Inhibition assay | IC50 = 1.50528 μM | SANGER | |||
| HN | Growth Inhibition assay | IC50 = 1.54071 μM | SANGER | |||
| NCI-H441 | Growth Inhibition assay | IC50 = 1.54907 μM | SANGER | |||
| RPMI-8866 | Growth Inhibition assay | IC50 = 1.58507 μM | SANGER | |||
| CAL-62 | Growth Inhibition assay | IC50 = 1.60862 μM | SANGER | |||
| MG-63 | Growth Inhibition assay | IC50 = 1.61813 μM | SANGER | |||
| SK-LU-1 | Growth Inhibition assay | IC50 = 1.62152 μM | SANGER | |||
| BCPAP | Growth Inhibition assay | IC50 = 1.66457 μM | SANGER | |||
| 22RV1 | Growth Inhibition assay | IC50 = 1.67843 μM | SANGER | |||
| T47D | Growth Inhibition assay | IC50 = 1.68061 μM | SANGER | |||
| MSTO-211H | Growth Inhibition assay | IC50 = 1.69603 μM | SANGER | |||
| DEL | Growth Inhibition assay | IC50 = 1.70273 μM | SANGER | |||
| H4 | Growth Inhibition assay | IC50 = 1.73212 μM | SANGER | |||
| CAL-51 | Growth Inhibition assay | IC50 = 1.74855 μM | SANGER | |||
| ABC-1 | Growth Inhibition assay | IC50 = 1.78582 μM | SANGER | |||
| MZ2-MEL | Growth Inhibition assay | IC50 = 1.79542 μM | SANGER | |||
| YKG-1 | Growth Inhibition assay | IC50 = 1.81061 μM | SANGER | |||
| KM12 | Growth Inhibition assay | IC50 = 1.81602 μM | SANGER | |||
| L-363 | Growth Inhibition assay | IC50 = 1.87412 μM | SANGER | |||
| KU812 | Growth Inhibition assay | IC50 = 1.89282 μM | SANGER | |||
| LOXIMVI | Growth Inhibition assay | IC50 = 1.91228 μM | SANGER | |||
| G-401 | Growth Inhibition assay | IC50 = 1.92428 μM | SANGER | |||
| SW780 | Growth Inhibition assay | IC50 = 1.96246 μM | SANGER | |||
| SW872 | Growth Inhibition assay | IC50 = 1.9833 μM | SANGER | |||
| NB7 | Growth Inhibition assay | IC50 = 1.99323 μM | SANGER | |||
| T98G | Growth Inhibition assay | IC50 = 2.00666 μM | SANGER | |||
| SW1710 | Growth Inhibition assay | IC50 = 2.06945 μM | SANGER | |||
| NCI-H1573 | Growth Inhibition assay | IC50 = 2.07298 μM | SANGER | |||
| KE-37 | Growth Inhibition assay | IC50 = 2.08951 μM | SANGER | |||
| 786-0 | Growth Inhibition assay | IC50 = 2.15439 μM | SANGER | |||
| SAS | Growth Inhibition assay | IC50 = 2.20374 μM | SANGER | |||
| CAL-54 | Growth Inhibition assay | IC50 = 2.20413 μM | SANGER | |||
| SF268 | Growth Inhibition assay | IC50 = 2.23122 μM | SANGER | |||
| SW620 | Growth Inhibition assay | IC50 = 2.26169 μM | SANGER | |||
| MN-60 | Growth Inhibition assay | IC50 = 2.3106 μM | SANGER | |||
| EFO-27 | Growth Inhibition assay | IC50 = 2.32058 μM | SANGER | |||
| NCI-H747 | Growth Inhibition assay | IC50 = 2.32199 μM | SANGER | |||
| HCC2218 | Growth Inhibition assay | IC50 = 2.35374 μM | SANGER | |||
| MIA-PaCa-2 | Growth Inhibition assay | IC50 = 2.36437 μM | SANGER | |||
| SJSA-1 | Growth Inhibition assay | IC50 = 2.37796 μM | SANGER | |||
| RKO | Growth Inhibition assay | IC50 = 2.38496 μM | SANGER | |||
| NB6 | Growth Inhibition assay | IC50 = 2.40374 μM | SANGER | |||
| ES4 | Growth Inhibition assay | IC50 = 2.45422 μM | SANGER | |||
| EGI-1 | Growth Inhibition assay | IC50 = 2.46883 μM | SANGER | |||
| CTV-1 | Growth Inhibition assay | IC50 = 2.52773 μM | SANGER | |||
| NCI-H1355 | Growth Inhibition assay | IC50 = 2.55951 μM | SANGER | |||
| GT3TKB | Growth Inhibition assay | IC50 = 2.59199 μM | SANGER | |||
| SK-HEP-1 | Growth Inhibition assay | IC50 = 2.59266 μM | SANGER | |||
| GAMG | Growth Inhibition assay | IC50 = 2.59394 μM | SANGER | |||
| SK-MES-1 | Growth Inhibition assay | IC50 = 2.61803 μM | SANGER | |||
| RO82-W-1 | Growth Inhibition assay | IC50 = 2.62057 μM | SANGER | |||
| ECC10 | Growth Inhibition assay | IC50 = 2.70206 μM | SANGER | |||
| MCF7 | Growth Inhibition assay | IC50 = 2.71464 μM | SANGER | |||
| D-283MED | Growth Inhibition assay | IC50 = 2.7243 μM | SANGER | |||
| RPMI-7951 | Growth Inhibition assay | IC50 = 2.75694 μM | SANGER | |||
| Ramos-2G6-4C10 | Growth Inhibition assay | IC50 = 2.77099 μM | SANGER | |||
| KGN | Growth Inhibition assay | IC50 = 2.81884 μM | SANGER | |||
| NUGC-3 | Growth Inhibition assay | IC50 = 2.82505 μM | SANGER | |||
| NCI-H292 | Growth Inhibition assay | IC50 = 2.85053 μM | SANGER | |||
| Becker | Growth Inhibition assay | IC50 = 2.95832 μM | SANGER | |||
| NCI-H1299 | Growth Inhibition assay | IC50 = 3.05263 μM | SANGER | |||
| ETK-1 | Growth Inhibition assay | IC50 = 3.0543 μM | SANGER | |||
| TK10 | Growth Inhibition assay | IC50 = 3.20165 μM | SANGER | |||
| VMRC-RCZ | Growth Inhibition assay | IC50 = 3.36488 μM | SANGER | |||
| YH-13 | Growth Inhibition assay | IC50 = 3.44079 μM | SANGER | |||
| DU-145 | Growth Inhibition assay | IC50 = 3.46269 μM | SANGER | |||
| SW1088 | Growth Inhibition assay | IC50 = 3.4747 μM | SANGER | |||
| HOP-92 | Growth Inhibition assay | IC50 = 3.50342 μM | SANGER | |||
| KP-N-YS | Growth Inhibition assay | IC50 = 3.62139 μM | SANGER | |||
| NCI-H460 | Growth Inhibition assay | IC50 = 3.6673 μM | SANGER | |||
| U-2-OS | Growth Inhibition assay | IC50 = 3.72535 μM | SANGER | |||
| A101D | Growth Inhibition assay | IC50 = 3.76936 μM | SANGER | |||
| MDA-MB-231 | Growth Inhibition assay | IC50 = 3.81951 μM | SANGER | |||
| IST-MES1 | Growth Inhibition assay | IC50 = 3.832 μM | SANGER | |||
| COR-L105 | Growth Inhibition assay | IC50 = 4.018 μM | SANGER | |||
| NCI-H1437 | Growth Inhibition assay | IC50 = 4.02302 μM | SANGER | |||
| CAL-85-1 | Growth Inhibition assay | IC50 = 4.02461 μM | SANGER | |||
| MZ1-PC | Growth Inhibition assay | IC50 = 4.18556 μM | SANGER | |||
| VM-CUB-1 | Growth Inhibition assay | IC50 = 4.31284 μM | SANGER | |||
| CHL-1 | Growth Inhibition assay | IC50 = 4.32169 μM | SANGER | |||
| MDA-MB-361 | Growth Inhibition assay | IC50 = 4.33153 μM | SANGER | |||
| NCI-H661 | Growth Inhibition assay | IC50 = 4.50092 μM | SANGER | |||
| EW-11 | Growth Inhibition assay | IC50 = 4.52231 μM | SANGER | |||
| BEN | Growth Inhibition assay | IC50 = 4.52815 μM | SANGER | |||
| BFTC-909 | Growth Inhibition assay | IC50 = 4.56275 μM | SANGER | |||
| NCI-H2087 | Growth Inhibition assay | IC50 = 4.58164 μM | SANGER | |||
| RVH-421 | Growth Inhibition assay | IC50 = 4.6669 μM | SANGER | |||
| P30-OHK | Growth Inhibition assay | IC50 = 4.68008 μM | SANGER | |||
| NCI-H28 | Growth Inhibition assay | IC50 = 4.81661 μM | SANGER | |||
| ES6 | Growth Inhibition assay | IC50 = 4.83016 μM | SANGER | |||
| 769-P | Growth Inhibition assay | IC50 = 4.85926 μM | SANGER | |||
| OE33 | Growth Inhibition assay | IC50 = 4.88161 μM | SANGER | |||
| SW982 | Growth Inhibition assay | IC50 = 4.95061 μM | SANGER | |||
| A388 | Growth Inhibition assay | IC50 = 5.02983 μM | SANGER | |||
| TI-73 | Growth Inhibition assay | IC50 = 5.06194 μM | SANGER | |||
| HCT-116 | Growth Inhibition assay | IC50 = 5.09889 μM | SANGER | |||
| HuP-T3 | Growth Inhibition assay | IC50 = 5.18709 μM | SANGER | |||
| G-402 | Growth Inhibition assay | IC50 = 5.19416 μM | SANGER | |||
| NCI-H1792 | Growth Inhibition assay | IC50 = 5.24622 μM | SANGER | |||
| NCI-H209 | Growth Inhibition assay | IC50 = 5.25942 μM | SANGER | |||
| NCI-H1650 | Growth Inhibition assay | IC50 = 5.30634 μM | SANGER | |||
| LCLC-97TM1 | Growth Inhibition assay | IC50 = 5.31808 μM | SANGER | |||
| S-117 | Growth Inhibition assay | IC50 = 5.36976 μM | SANGER | |||
| GI-ME-N | Growth Inhibition assay | IC50 = 5.39681 μM | SANGER | |||
| NCI-H2122 | Growth Inhibition assay | IC50 = 5.49397 μM | SANGER | |||
| NCI-H1793 | Growth Inhibition assay | IC50 = 5.67593 μM | SANGER | |||
| C2BBe1 | Growth Inhibition assay | IC50 = 5.70088 μM | SANGER | |||
| TE-12 | Growth Inhibition assay | IC50 = 5.80556 μM | SANGER | |||
| LCLC-103H | Growth Inhibition assay | IC50 = 5.917 μM | SANGER | |||
| A673 | Growth Inhibition assay | IC50 = 5.91932 μM | SANGER | |||
| BB30-HNC | Growth Inhibition assay | IC50 = 5.9836 μM | SANGER | |||
| SF295 | Growth Inhibition assay | IC50 = 6.00422 μM | SANGER | |||
| KU-19-19 | Growth Inhibition assay | IC50 = 6.01731 μM | SANGER | |||
| CFPAC-1 | Growth Inhibition assay | IC50 = 6.04443 μM | SANGER | |||
| LoVo | Growth Inhibition assay | IC50 = 6.05063 μM | SANGER | |||
| 8505C | Growth Inhibition assay | IC50 = 6.07573 μM | SANGER | |||
| GMS-10 | Growth Inhibition assay | IC50 = 6.15002 μM | SANGER | |||
| Ca9-22 | Growth Inhibition assay | IC50 = 6.1671 μM | SANGER | |||
| DOK | Growth Inhibition assay | IC50 = 6.22072 μM | SANGER | |||
| FADU | Growth Inhibition assay | IC50 = 6.26039 μM | SANGER | |||
| BxPC-3 | Growth Inhibition assay | IC50 = 6.2732 μM | SANGER | |||
| CAL-33 | Growth Inhibition assay | IC50 = 6.29201 μM | SANGER | |||
| SHP-77 | Growth Inhibition assay | IC50 = 6.31512 μM | SANGER | |||
| LXF-289 | Growth Inhibition assay | IC50 = 6.33455 μM | SANGER | |||
| GB-1 | Growth Inhibition assay | IC50 = 6.382 μM | SANGER | |||
| KS-1 | Growth Inhibition assay | IC50 = 6.38447 μM | SANGER | |||
| D-502MG | Growth Inhibition assay | IC50 = 6.42376 μM | SANGER | |||
| LAN-6 | Growth Inhibition assay | IC50 = 6.51023 μM | SANGER | |||
| H-EMC-SS | Growth Inhibition assay | IC50 = 6.56147 μM | SANGER | |||
| LC-2-ad | Growth Inhibition assay | IC50 = 6.60076 μM | SANGER | |||
| NCI-H1693 | Growth Inhibition assay | IC50 = 6.62215 μM | SANGER | |||
| SK-N-FI | Growth Inhibition assay | IC50 = 6.75044 μM | SANGER | |||
| D-423MG | Growth Inhibition assay | IC50 = 6.76117 μM | SANGER | |||
| KNS-42 | Growth Inhibition assay | IC50 = 6.78197 μM | SANGER | |||
| GCT | Growth Inhibition assay | IC50 = 6.938 μM | SANGER | |||
| DSH1 | Growth Inhibition assay | IC50 = 7.0633 μM | SANGER | |||
| D-247MG | Growth Inhibition assay | IC50 = 7.07881 μM | SANGER | |||
| NCI-SNU-5 | Growth Inhibition assay | IC50 = 7.18371 μM | SANGER | |||
| TE-6 | Growth Inhibition assay | IC50 = 7.20601 μM | SANGER | |||
| NOMO-1 | Growth Inhibition assay | IC50 = 7.22127 μM | SANGER | |||
| NB17 | Growth Inhibition assay | IC50 = 7.30309 μM | SANGER | |||
| EW-22 | Growth Inhibition assay | IC50 = 7.34348 μM | SANGER | |||
| EW-13 | Growth Inhibition assay | IC50 = 7.35162 μM | SANGER | |||
| DOHH-2 | Growth Inhibition assay | IC50 = 7.4402 μM | SANGER | |||
| TGBC1TKB | Growth Inhibition assay | IC50 = 7.49899 μM | SANGER | |||
| GR-ST | Growth Inhibition assay | IC50 = 7.52594 μM | SANGER | |||
| KYSE-520 | Growth Inhibition assay | IC50 = 7.55515 μM | SANGER | |||
| CAPAN-1 | Growth Inhibition assay | IC50 = 7.5951 μM | SANGER | |||
| HCE-4 | Growth Inhibition assay | IC50 = 7.62279 μM | SANGER | |||
| MLMA | Growth Inhibition assay | IC50 = 7.62957 μM | SANGER | |||
| HT-144 | Growth Inhibition assay | IC50 = 7.65368 μM | SANGER | |||
| KYSE-180 | Growth Inhibition assay | IC50 = 7.71169 μM | SANGER | |||
| TE-5 | Growth Inhibition assay | IC50 = 7.95971 μM | SANGER | |||
| IGROV-1 | Growth Inhibition assay | IC50 = 7.98551 μM | SANGER | |||
| NCI-H1581 | Growth Inhibition assay | IC50 = 8.012 μM | SANGER | |||
| SW1990 | Growth Inhibition assay | IC50 = 8.04659 μM | SANGER | |||
| EFM-19 | Growth Inhibition assay | IC50 = 8.08545 μM | SANGER | |||
| IGR-1 | Growth Inhibition assay | IC50 = 8.43023 μM | SANGER | |||
| U-118-MG | Growth Inhibition assay | IC50 = 8.43463 μM | SANGER | |||
| SK-OV-3 | Growth Inhibition assay | IC50 = 8.46765 μM | SANGER | |||
| KNS-62 | Growth Inhibition assay | IC50 = 8.51761 μM | SANGER | |||
| GOTO | Growth Inhibition assay | IC50 = 8.57635 μM | SANGER | |||
| 8305C | Growth Inhibition assay | IC50 = 8.70484 μM | SANGER | |||
| RPMI-2650 | Growth Inhibition assay | IC50 = 8.71955 μM | SANGER | |||
| NEC8 | Growth Inhibition assay | IC50 = 8.74307 μM | SANGER | |||
| KYSE-450 | Growth Inhibition assay | IC50 = 8.86548 μM | SANGER | |||
| RMG-I | Growth Inhibition assay | IC50 = 9.14058 μM | SANGER | |||
| CAKI-1 | Growth Inhibition assay | IC50 = 9.31979 μM | SANGER | |||
| KYSE-510 | Growth Inhibition assay | IC50 = 9.35778 μM | SANGER | |||
| A4-Fuk | Growth Inhibition assay | IC50 = 9.36701 μM | SANGER | |||
| AN3-CA | Growth Inhibition assay | IC50 = 9.45444 μM | SANGER | |||
| SK-N-DZ | Growth Inhibition assay | IC50 = 9.72849 μM | SANGER | |||
| HSC-2 | Growth Inhibition assay | IC50 = 9.76629 μM | SANGER | |||
| EW-1 | Growth Inhibition assay | IC50 = 9.79369 μM | SANGER | |||
| D-566MG | Growth Inhibition assay | IC50 = 9.83664 μM | SANGER | |||
| COLO-792 | Growth Inhibition assay | IC50 = 9.98746 μM | SANGER | |||
| TE-10 | Growth Inhibition assay | IC50 = 10.0396 μM | SANGER | |||
| NCI-H650 | Growth Inhibition assay | IC50 = 10.4286 μM | SANGER | |||
| U-266 | Growth Inhibition assay | IC50 = 10.455 μM | SANGER | |||
| Detroit562 | Growth Inhibition assay | IC50 = 11.0515 μM | SANGER | |||
| NH-12 | Growth Inhibition assay | IC50 = 11.1446 μM | SANGER | |||
| OC-314 | Growth Inhibition assay | IC50 = 11.2842 μM | SANGER | |||
| IST-MEL1 | Growth Inhibition assay | IC50 = 11.5323 μM | SANGER | |||
| KNS-81-FD | Growth Inhibition assay | IC50 = 11.5527 μM | SANGER | |||
| SW1463 | Growth Inhibition assay | IC50 = 11.5989 μM | SANGER | |||
| NCI-H23 | Growth Inhibition assay | IC50 = 11.6553 μM | SANGER | |||
| SK-MEL-2 | Growth Inhibition assay | IC50 = 11.7197 μM | SANGER | |||
| NB13 | Growth Inhibition assay | IC50 = 12.1495 μM | SANGER | |||
| Daoy | Growth Inhibition assay | IC50 = 12.2855 μM | SANGER | |||
| NCI-H1623 | Growth Inhibition assay | IC50 = 12.3801 μM | SANGER | |||
| NMC-G1 | Growth Inhibition assay | IC50 = 12.717 μM | SANGER | |||
| DK-MG | Growth Inhibition assay | IC50 = 12.9482 μM | SANGER | |||
| TCCSUP | Growth Inhibition assay | IC50 = 13.1284 μM | SANGER | |||
| SCC-15 | Growth Inhibition assay | IC50 = 13.2651 μM | SANGER | |||
| NOS-1 | Growth Inhibition assay | IC50 = 13.2893 μM | SANGER | |||
| RH-1 | Growth Inhibition assay | IC50 = 13.3037 μM | SANGER | |||
| SK-MEL-3 | Growth Inhibition assay | IC50 = 13.3728 μM | SANGER | |||
| NB5 | Growth Inhibition assay | IC50 = 13.4067 μM | SANGER | |||
| SNU-387 | Growth Inhibition assay | IC50 = 13.5072 μM | SANGER | |||
| CAL-120 | Growth Inhibition assay | IC50 = 13.6718 μM | SANGER | |||
| LNCaP-Clone-FGC | Growth Inhibition assay | IC50 = 13.7991 μM | SANGER | |||
| ACN | Growth Inhibition assay | IC50 = 14.0288 μM | SANGER | |||
| SK-MEL-30 | Growth Inhibition assay | IC50 = 14.063 μM | SANGER | |||
| COLO-678 | Growth Inhibition assay | IC50 = 14.0822 μM | SANGER | |||
| SCC-9 | Growth Inhibition assay | IC50 = 14.1021 μM | SANGER | |||
| KINGS-1 | Growth Inhibition assay | IC50 = 14.1402 μM | SANGER | |||
| LS-513 | Growth Inhibition assay | IC50 = 14.187 μM | SANGER | |||
| HLE | Growth Inhibition assay | IC50 = 14.3852 μM | SANGER | |||
| SW1573 | Growth Inhibition assay | IC50 = 14.4435 μM | SANGER | |||
| KYSE-140 | Growth Inhibition assay | IC50 = 14.6327 μM | SANGER | |||
| SK-PN-DW | Growth Inhibition assay | IC50 = 14.8001 μM | SANGER | |||
| A253 | Growth Inhibition assay | IC50 = 15.0625 μM | SANGER | |||
| CAL-12T | Growth Inhibition assay | IC50 = 15.4662 μM | SANGER | |||
| COLO-679 | Growth Inhibition assay | IC50 = 15.7683 μM | SANGER | |||
| UACC-257 | Growth Inhibition assay | IC50 = 16.1201 μM | SANGER | |||
| U-87-MG | Growth Inhibition assay | IC50 = 16.3523 μM | SANGER | |||
| HCC1806 | Growth Inhibition assay | IC50 = 16.7071 μM | SANGER | |||
| NCI-H2170 | Growth Inhibition assay | IC50 = 17.2448 μM | SANGER | |||
| AGS | Growth Inhibition assay | IC50 = 17.3808 μM | SANGER | |||
| MEL-HO | Growth Inhibition assay | IC50 = 17.7503 μM | SANGER | |||
| SW48 | Growth Inhibition assay | IC50 = 17.7716 μM | SANGER | |||
| HuP-T4 | Growth Inhibition assay | IC50 = 18.0206 μM | SANGER | |||
| NCI-H720 | Growth Inhibition assay | IC50 = 18.1402 μM | SANGER | |||
| RCC10RGB | Growth Inhibition assay | IC50 = 18.1697 μM | SANGER | |||
| HD-MY-Z | Growth Inhibition assay | IC50 = 18.2254 μM | SANGER | |||
| A427 | Growth Inhibition assay | IC50 = 18.5094 μM | SANGER | |||
| HCC2998 | Growth Inhibition assay | IC50 = 18.6051 μM | SANGER | |||
| EPLC-272H | Growth Inhibition assay | IC50 = 19.0434 μM | SANGER | |||
| C32 | Growth Inhibition assay | IC50 = 19.045 μM | SANGER | |||
| UMC-11 | Growth Inhibition assay | IC50 = 19.2123 μM | SANGER | |||
| CaR-1 | Growth Inhibition assay | IC50 = 19.6804 μM | SANGER | |||
| KYSE-410 | Growth Inhibition assay | IC50 = 19.9139 μM | SANGER | |||
| HuCCT1 | Growth Inhibition assay | IC50 = 20.6293 μM | SANGER | |||
| LB996-RCC | Growth Inhibition assay | IC50 = 20.7168 μM | SANGER | |||
| KYSE-70 | Growth Inhibition assay | IC50 = 20.8059 μM | SANGER | |||
| CAL-72 | Growth Inhibition assay | IC50 = 20.915 μM | SANGER | |||
| Capan-2 | Growth Inhibition assay | IC50 = 21.0413 μM | SANGER | |||
| PANC-08-13 | Growth Inhibition assay | IC50 = 21.2515 μM | SANGER | |||
| SBC-1 | Growth Inhibition assay | IC50 = 21.3081 μM | SANGER | |||
| MFM-223 | Growth Inhibition assay | IC50 = 21.3342 μM | SANGER | |||
| BB49-HNC | Growth Inhibition assay | IC50 = 21.5716 μM | SANGER | |||
| SH-4 | Growth Inhibition assay | IC50 = 21.6618 μM | SANGER | |||
| HuO9 | Growth Inhibition assay | IC50 = 21.9825 μM | SANGER | |||
| AM-38 | Growth Inhibition assay | IC50 = 22.0485 μM | SANGER | |||
| A431 | Growth Inhibition assay | IC50 = 23.2119 μM | SANGER | |||
| YAPC | Growth Inhibition assay | IC50 = 23.2651 μM | SANGER | |||
| LU-139 | Growth Inhibition assay | IC50 = 23.4809 μM | SANGER | |||
| HEC-1 | Growth Inhibition assay | IC50 = 23.4937 μM | SANGER | |||
| SCC-25 | Growth Inhibition assay | IC50 = 24.3006 μM | SANGER | |||
| HT-29 | Growth Inhibition assay | IC50 = 24.3823 μM | SANGER | |||
| PC-14 | Growth Inhibition assay | IC50 = 24.6571 μM | SANGER | |||
| Calu-6 | Growth Inhibition assay | IC50 = 25.5071 μM | SANGER | |||
| SJRH30 | Growth Inhibition assay | IC50 = 25.6496 μM | SANGER | |||
| ChaGo-K-1 | Growth Inhibition assay | IC50 = 26.1629 μM | SANGER | |||
| IA-LM | Growth Inhibition assay | IC50 = 26.3645 μM | SANGER | |||
| GP5d | Growth Inhibition assay | IC50 = 26.4491 μM | SANGER | |||
| NCI-H2291 | Growth Inhibition assay | IC50 = 26.6541 μM | SANGER | |||
| BALL-1 | Growth Inhibition assay | IC50 = 26.9397 μM | SANGER | |||
| HCC1954 | Growth Inhibition assay | IC50 = 26.9808 μM | SANGER | |||
| NCI-H2452 | Growth Inhibition assay | IC50 = 27.4163 μM | SANGER | |||
| LU-99A | Growth Inhibition assay | IC50 = 27.5582 μM | SANGER | |||
| NTERA-S-cl-D1 | Growth Inhibition assay | IC50 = 27.7299 μM | SANGER | |||
| PANC-10-05 | Growth Inhibition assay | IC50 = 27.7775 μM | SANGER | |||
| NCI-H2405 | Growth Inhibition assay | IC50 = 27.9387 μM | SANGER | |||
| MDA-MB-415 | Growth Inhibition assay | IC50 = 28.4137 μM | SANGER | |||
| NCI-H2342 | Growth Inhibition assay | IC50 = 28.5281 μM | SANGER | |||
| TGBC24TKB | Growth Inhibition assay | IC50 = 28.7117 μM | SANGER | |||
| LU-134-A | Growth Inhibition assay | IC50 = 28.9261 μM | SANGER | |||
| SCC-4 | Growth Inhibition assay | IC50 = 31.0495 μM | SANGER | |||
| Saos-2 | Growth Inhibition assay | IC50 = 31.9306 μM | SANGER | |||
| RERF-LC-MS | Growth Inhibition assay | IC50 = 32.8231 μM | SANGER | |||
| M14 | Growth Inhibition assay | IC50 = 32.9764 μM | SANGER | |||
| HPAF-II | Growth Inhibition assay | IC50 = 33.5011 μM | SANGER | |||
| NCI-H1755 | Growth Inhibition assay | IC50 = 34.3305 μM | SANGER | |||
| D-392MG | Growth Inhibition assay | IC50 = 35.8674 μM | SANGER | |||
| A704 | Growth Inhibition assay | IC50 = 36.0427 μM | SANGER | |||
| CP50-MEL-B | Growth Inhibition assay | IC50 = 36.1911 μM | SANGER | |||
| EW-18 | Growth Inhibition assay | IC50 = 36.452 μM | SANGER | |||
| WM-115 | Growth Inhibition assay | IC50 = 36.8099 μM | SANGER | |||
| LU-65 | Growth Inhibition assay | IC50 = 37.1417 μM | SANGER | |||
| NCI-H1563 | Growth Inhibition assay | IC50 = 37.2484 μM | SANGER | |||
| DBTRG-05MG | Growth Inhibition assay | IC50 = 38.0691 μM | SANGER | |||
| NCI-H630 | Growth Inhibition assay | IC50 = 38.4714 μM | SANGER | |||
| NCI-H1155 | Growth Inhibition assay | IC50 = 39.242 μM | SANGER | |||
| OVCAR-3 | Growth Inhibition assay | IC50 = 39.9195 μM | SANGER | |||
| OAW-42 | Growth Inhibition assay | IC50 = 40.4258 μM | SANGER | |||
| JVM-2 | Growth Inhibition assay | IC50 = 41.2415 μM | SANGER | |||
| C3A | Growth Inhibition assay | IC50 = 41.3447 μM | SANGER | |||
| HT55 | Growth Inhibition assay | IC50 = 42.2841 μM | SANGER | |||
| OVCAR-4 | Growth Inhibition assay | IC50 = 42.2974 μM | SANGER | |||
| MEG-01 | Growth Inhibition assay | IC50 = 42.4616 μM | SANGER | |||
| NCI-H82 | Growth Inhibition assay | IC50 = 43.9892 μM | SANGER | |||
| JEG-3 | Growth Inhibition assay | IC50 = 44.947 μM | SANGER | |||
| BPH-1 | Growth Inhibition assay | IC50 = 46.3998 μM | SANGER | |||
| MPP-89 | Growth Inhibition assay | IC50 = 47.2898 μM | SANGER | |||
| ALL-PO | Growth Inhibition assay | IC50 = 47.4188 μM | SANGER | |||
| HT | Growth Inhibition assay | IC50 = 47.492 μM | SANGER | |||
| NCI-H2347 | Growth Inhibition assay | IC50 = 48.0715 μM | SANGER | |||
| A2780 | Growth Inhibition assay | IC50 = 49.4228 μM | SANGER | |||
| KARPAS-299 | Growth Inhibition assay | IC50 = 49.5119 μM | SANGER | |||
| NCI-H1651 | Growth Inhibition assay | IC50 = 49.8821 μM | SANGER | |||
| OCI-AML2 | Growth Inhibition assay | IC50 = 50.2084 μM | SANGER | |||
| OCUB-M | Growth Inhibition assay | IC50 = 50.3047 μM | SANGER | |||
| HuH-7 | Growth Inhibition assay | IC50 = 50.5943 μM | SANGER | |||
| RCM-1 | Growth Inhibition assay | IC50 = 50.9133 μM | SANGER | |||
| FTC-133 | Growth Inhibition assay | IC50 = 51.322 μM | SANGER | |||
| PSN1 | Growth Inhibition assay | IC50 = 51.4335 μM | SANGER | |||
| A498 | Growth Inhibition assay | IC50 = 52.0995 μM | SANGER | |||
| SF126 | Growth Inhibition assay | IC50 = 52.6568 μM | SANGER | |||
| UACC-62 | Growth Inhibition assay | IC50 = 55.2224 μM | SANGER | |||
| PANC-03-27 | Growth Inhibition assay | IC50 = 56.6788 μM | SANGER | |||
| NCI-H727 | Growth Inhibition assay | IC50 = 56.8127 μM | SANGER | |||
| SNU-423 | Growth Inhibition assay | IC50 = 57.2859 μM | SANGER | |||
| LB771-HNC | Growth Inhibition assay | IC50 = 57.8405 μM | SANGER | |||
| HCC1395 | Growth Inhibition assay | IC50 = 58.0464 μM | SANGER | |||
| OAW-28 | Growth Inhibition assay | IC50 = 58.2785 μM | SANGER | |||
| NB12 | Growth Inhibition assay | IC50 = 60.6696 μM | SANGER | |||
| DJM-1 | Growth Inhibition assay | IC50 = 60.7331 μM | SANGER | |||
| MDA-MB-157 | Growth Inhibition assay | IC50 = 61.1649 μM | SANGER | |||
| DU-4475 | Growth Inhibition assay | IC50 = 62.5495 μM | SANGER | |||
| RD | Growth Inhibition assay | IC50 = 62.7387 μM | SANGER | |||
| LS-123 | Growth Inhibition assay | IC50 = 63.2618 μM | SANGER | |||
| NCI-H226 | Growth Inhibition assay | IC50 = 64.22 μM | SANGER | |||
| MS-1 | Growth Inhibition assay | IC50 = 64.8358 μM | SANGER | |||
| no-10 | Growth Inhibition assay | IC50 = 65.7473 μM | SANGER | |||
| SW626 | Growth Inhibition assay | IC50 = 65.7579 μM | SANGER | |||
| DMS-273 | Growth Inhibition assay | IC50 = 66.2296 μM | SANGER | |||
| ESS-1 | Growth Inhibition assay | IC50 = 66.5096 μM | SANGER | |||
| TE-9 | Growth Inhibition assay | IC50 = 66.6316 μM | SANGER | |||
| CAS-1 | Growth Inhibition assay | IC50 = 67.7954 μM | SANGER | |||
| 639-V | Growth Inhibition assay | IC50 = 69.4198 μM | SANGER | |||
| GAK | Growth Inhibition assay | IC50 = 70.2031 μM | SANGER | |||
| NCI-H526 | Growth Inhibition assay | IC50 = 71.0913 μM | SANGER | |||
| DoTc2-4510 | Growth Inhibition assay | IC50 = 71.443 μM | SANGER | |||
| 647-V | Growth Inhibition assay | IC50 = 73.2118 μM | SANGER | |||
| OVCAR-8 | Growth Inhibition assay | IC50 = 73.2367 μM | SANGER | |||
| COLO-680N | Growth Inhibition assay | IC50 = 75.2497 μM | SANGER | |||
| HDLM-2 | Growth Inhibition assay | IC50 = 75.7806 μM | SANGER | |||
| TGBC11TKB | Growth Inhibition assay | IC50 = 79.0192 μM | SANGER | |||
| DMS-114 | Growth Inhibition assay | IC50 = 81.9577 μM | SANGER | |||
| CW-2 | Growth Inhibition assay | IC50 = 82.6818 μM | SANGER | |||
| MDA-MB-175-VII | Growth Inhibition assay | IC50 = 85.3135 μM | SANGER | |||
| HT-1376 | Growth Inhibition assay | IC50 = 85.846 μM | SANGER | |||
| SW1417 | Growth Inhibition assay | IC50 = 88.2906 μM | SANGER | |||
| HCE-T | Growth Inhibition assay | IC50 = 91.7205 μM | SANGER | |||
| OE19 | Growth Inhibition assay | IC50 = 92.7944 μM | SANGER | |||
| NCI-N87 | Growth Inhibition assay | IC50 = 92.8881 μM | SANGER | |||
| SNU-449 | Growth Inhibition assay | IC50 = 93.584 μM | SANGER | |||
| NCI-H1092 | Growth Inhibition assay | IC50 = 96.5851 μM | SANGER | |||
| COLO-684 | Growth Inhibition assay | IC50 = 99.0686 μM | SANGER | |||
| HCC1937 | Growth Inhibition assay | IC50 = 99.9315 μM | SANGER | |||
| EFO-21 | Growth Inhibition assay | IC50 = 110.988 μM | SANGER | |||
| ZR-75-30 | Growth Inhibition assay | IC50 = 114.117 μM | SANGER | |||
| HCC1187 | Growth Inhibition assay | IC50 = 114.179 μM | SANGER | |||
| SW684 | Growth Inhibition assay | IC50 = 114.655 μM | SANGER | |||
| AU565 | Growth Inhibition assay | IC50 = 115.892 μM | SANGER | |||
| HCC38 | Growth Inhibition assay | IC50 = 116.559 μM | SANGER | |||
| LK-2 | Growth Inhibition assay | IC50 = 119.652 μM | SANGER | |||
| LB2518-MEL | Growth Inhibition assay | IC50 = 122.428 μM | SANGER | |||
| COLO-320-HSR | Growth Inhibition assay | IC50 = 126.212 μM | SANGER | |||
| HCC1419 | Growth Inhibition assay | IC50 = 129.227 μM | SANGER | |||
| NCI-H2228 | Growth Inhibition assay | IC50 = 129.321 μM | SANGER | |||
| NCI-H2052 | Growth Inhibition assay | IC50 = 130.358 μM | SANGER | |||
| HCC2157 | Growth Inhibition assay | IC50 = 133.973 μM | SANGER | |||
| HCC1569 | Growth Inhibition assay | IC50 = 135.05 μM | SANGER | |||
| HuO-3N1 | Growth Inhibition assay | IC50 = 135.366 μM | SANGER | |||
| MZ7-mel | Growth Inhibition assay | IC50 = 145.604 μM | SANGER | |||
| SW756 | Growth Inhibition assay | IC50 = 147.143 μM | SANGER | |||
| NCI-H1304 | Growth Inhibition assay | IC50 = 149.222 μM | SANGER | |||
| LN-405 | Growth Inhibition assay | IC50 = 149.732 μM | SANGER | |||
| BT-474 | Growth Inhibition assay | IC50 = 150.969 μM | SANGER | |||
| LS-411N | Growth Inhibition assay | IC50 = 152.319 μM | SANGER | |||
| ATN-1 | Growth Inhibition assay | IC50 = 152.458 μM | SANGER | |||
| SNU-C2B | Growth Inhibition assay | IC50 = 153.444 μM | SANGER | |||
| KYSE-270 | Growth Inhibition assay | IC50 = 155.75 μM | SANGER | |||
| NCI-H1395 | Growth Inhibition assay | IC50 = 156.493 μM | SANGER | |||
| EKVX | Growth Inhibition assay | IC50 = 156.981 μM | SANGER | |||
| HCC70 | Growth Inhibition assay | IC50 = 157.989 μM | SANGER | |||
| NCI-H522 | Growth Inhibition assay | IC50 = 161.368 μM | SANGER | |||
| Ca-Ski | Growth Inhibition assay | IC50 = 161.86 μM | SANGER | |||
| SW1116 | Growth Inhibition assay | IC50 = 163.382 μM | SANGER | |||
| 8-MG-BA | Growth Inhibition assay | IC50 = 165.797 μM | SANGER | |||
| NCI-H1048 | Growth Inhibition assay | IC50 = 172.374 μM | SANGER | |||
| RH-18 | Growth Inhibition assay | IC50 = 172.601 μM | SANGER | |||
| LU-135 | Growth Inhibition assay | IC50 = 173.259 μM | SANGER | |||
| SW948 | Growth Inhibition assay | IC50 = 174.6 μM | SANGER | |||
| LS-1034 | Growth Inhibition assay | IC50 = 183.742 μM | SANGER | |||
| SCH | Growth Inhibition assay | IC50 = 187.022 μM | SANGER | |||
| KP-N-YN | Growth Inhibition assay | IC50 = 192.971 μM | SANGER | |||
| NCI-H69 | Growth Inhibition assay | IC50 = 210.925 μM | SANGER | |||
| SBC-5 | Growth Inhibition assay | IC50 = 211.162 μM | SANGER | |||
| MFE-280 | Growth Inhibition assay | IC50 = 212.067 μM | SANGER | |||
| MC116 | Growth Inhibition assay | IC50 = 212.736 μM | SANGER | |||
| BT-20 | Growth Inhibition assay | IC50 = 216.38 μM | SANGER | |||
| NCI-H1993 | Growth Inhibition assay | IC50 = 217.295 μM | SANGER | |||
| Calu-3 | Growth Inhibition assay | IC50 = 217.37 μM | SANGER | |||
| GCIY | Growth Inhibition assay | IC50 = 221.332 μM | SANGER | |||
| HT-3 | Growth Inhibition assay | IC50 = 222.173 μM | SANGER | |||
| MC-IXC | Growth Inhibition assay | IC50 = 227.215 μM | SANGER | |||
| COR-L88 | Growth Inhibition assay | IC50 = 234.259 μM | SANGER | |||
| SK-MEL-1 | Growth Inhibition assay | IC50 = 235.59 μM | SANGER | |||
| MDA-MB-453 | Growth Inhibition assay | IC50 = 236.33 μM | SANGER | |||
| SiHa | Growth Inhibition assay | IC50 = 247.22 μM | SANGER | |||
| C8166 | Growth Inhibition assay | IC50 = 251.341 μM | SANGER | |||
| SKG-IIIa | Growth Inhibition assay | IC50 = 251.504 μM | SANGER | |||
| HT-1197 | Growth Inhibition assay | IC50 = 268.492 μM | SANGER | |||
| no-11 | Growth Inhibition assay | IC50 = 291.357 μM | SANGER | |||
| ME-180 | Growth Inhibition assay | IC50 = 296.912 μM | SANGER | |||
| NY | Growth Inhibition assay | IC50 = 320.632 μM | SANGER | |||
| C-33-A | Growth Inhibition assay | IC50 = 325.06 μM | SANGER | |||
| NCI-H2029 | Growth Inhibition assay | IC50 = 338.305 μM | SANGER | |||
| IST-SL1 | Growth Inhibition assay | IC50 = 342.105 μM | SANGER | |||
| KLE | Growth Inhibition assay | IC50 = 347.29 μM | SANGER | |||
| SF539 | Growth Inhibition assay | IC50 = 348.01 μM | SANGER | |||
| 5637 | Growth Inhibition assay | IC50 = 360.37 μM | SANGER | |||
| COLO-824 | Growth Inhibition assay | IC50 = 363.58 μM | SANGER | |||
| NCI-H810 | Growth Inhibition assay | IC50 = 363.938 μM | SANGER | |||
| JAR | Growth Inhibition assay | IC50 = 365.01 μM | SANGER | |||
| L-428 | Growth Inhibition assay | IC50 = 369.277 μM | SANGER | |||
| COLO-668 | Growth Inhibition assay | IC50 = 387.033 μM | SANGER | |||
| GI-1 | Growth Inhibition assay | IC50 = 398.59 μM | SANGER | |||
| NCI-H446 | Growth Inhibition assay | IC50 = 399.497 μM | SANGER | |||
| CCRF-CEM | Growth Inhibition assay | IC50 = 403.587 μM | SANGER | |||
| T84 | Growth Inhibition assay | IC50 = 403.686 μM | SANGER | |||
| K-562 | Growth Inhibition assay | IC50 = 432.947 μM | SANGER | |||
| OMC-1 | Growth Inhibition assay | IC50 = 433.814 μM | SANGER | |||
| LB831-BLC | Growth Inhibition assay | IC50 = 434.556 μM | SANGER | |||
| BT-549 | Growth Inhibition assay | IC50 = 435.102 μM | SANGER | |||
| MKN7 | Growth Inhibition assay | IC50 = 439.822 μM | SANGER | |||
| SW1783 | Growth Inhibition assay | IC50 = 449.251 μM | SANGER | |||
| SNB75 | Growth Inhibition assay | IC50 = 486.478 μM | SANGER | |||
| M059J | Growth Inhibition assay | IC50 = 492.923 μM | SANGER | |||
| KURAMOCHI | Growth Inhibition assay | IC50 = 498.612 μM | SANGER | |||
| TE-1 | Growth Inhibition assay | IC50 = 502.729 μM | SANGER | |||
| NCI-H596 | Growth Inhibition assay | IC50 = 530.805 μM | SANGER | |||
| PFSK-1 | Growth Inhibition assay | IC50 = 532.941 μM | SANGER | |||
| MOLM13 | Function assay | 24 hrs | Inhibition of CDK4 in human MOLM13 cells assessed as inhibition of Rb phosphorylation at Ser780 after 24 hrs, IC50 = 0.011 μM. | 24641103 | ||
| COLO205 | Antiproliferative assay | 72 hrs | Antiproliferative activity against Rb-positive human COLO205 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis, IC50 = 0.036 μM. | 24641103 | ||
| MOLM13 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis, IC50 = 0.096 μM. | 24641103 | ||
| MOLM13 | Antiproliferative assay | 72 hrs | Antiproliferative activity against sorafenib-resistant human MOLM13 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis, IC50 = 0.096 μM. | 24641103 | ||
| U937 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U937 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis, IC50 = 0.14 μM. | 24641103 | ||
| insect cell | Function assay | 2 mins | Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis, IC50 = 0.009 μM. | 26115571 | ||
| insect cell | Function assay | 2 mins | Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis, IC50 = 0.009 μM. | 26115571 | ||
| insect cell | Function assay | 2 mins | Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis, IC50 = 0.011 μM. | 26115571 | ||
| insect cell | Function assay | 2 mins | Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis, IC50 = 0.011 μM. | 26115571 | ||
| MDA-MB-435 | Antiproliferative assay | 24 hrs | Antiproliferative activity against Rb-positive human MDA-MB-435 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis, IC50 = 0.16 μM. | 26115571 | ||
| sf9 | Function assay | Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP, IC50 = 9.2 μM. | 26851505 | |||
| sf9 | Function assay | Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP, IC50 = 9.2 μM. | 26851505 | |||
| insect cell | Function assay | 2 mins | Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method, IC50 = 0.011 μM. | 27171036 | ||
| insect cell | Function assay | 2 mins | Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method, IC50 = 0.011 μM. | 27171036 | ||
| insect cell | Function assay | 2 mins | Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method, IC50 = 0.015 μM. | 27171036 | ||
| insect cell | Function assay | 2 mins | Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method, IC50 = 0.015 μM. | 27171036 | ||
| MDA-MB-453 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay, IC50 = 0.137 μM. | 27448913 | ||
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay, IC50 = 0.24 μM. | 27448913 | ||
| MDA-MB-231 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay, IC50 = 0.58 μM. | 27448913 | ||
| MCF7 | Antitumor assay | 100 mg/kg/day | 14 days | Antitumor activity against human estrogen-independent human MCF7 cells xenografted in RNU rat assessed as tumor growth inhibition at 100 mg/kg/day, ig administered for 14 days measured on day 15 | 27448913 | |
| A2780 | Growth inhibition assay | 72 hrs | Growth inhibition of human A2780 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.032 μM. | 28156111 | ||
| MV4-11 | Growth inhibition assay | 72 hrs | Growth inhibition of human MV4-11 cells after 72 hrs by resazurin assay, GI50 = 0.05 μM. | 28156111 | ||
| MOLM13 | Growth inhibition assay | 72 hrs | Growth inhibition of human MOLM13 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.062 μM. | 28156111 | ||
| NB4 | Growth inhibition assay | 72 hrs | Growth inhibition of human NB4 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.066 μM. | 28156111 | ||
| PC3 | Growth inhibition assay | 72 hrs | Growth inhibition of human PC3 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.071 μM. | 28156111 | ||
| MDA-MB-453 | Growth inhibition assay | 72 hrs | Growth inhibition of human MDA-MB-453 cells after 72 hrs by MTT assay, GI50 = 0.326 μM. | 28156111 | ||
| MCF7 | Growth inhibition assay | 72 hrs | Growth inhibition of human MCF7 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.557 μM. | 28156111 | ||
| M229 | Growth inhibition assay | 72 hrs | Growth inhibition of human M229 cells after 72 hrs by resazurin or MTT assay, GI50 = 1.22 μM. | 28156111 | ||
| M238 | Growth inhibition assay | 72 hrs | Growth inhibition of human M238 cells after 72 hrs by resazurin or MTT assay, GI50 = 1.97 μM. | 28156111 | ||
| M249 | Growth inhibition assay | 72 hrs | Growth inhibition of human M249 cells after 72 hrs by resazurin or MTT assay, GI50 = 1.99 μM. | 28156111 | ||
| M249R | Growth inhibition assay | 72 hrs | Growth inhibition of human M249R cells after 72 hrs by resazurin or MTT assay, GI50 = 2.96 μM. | 28156111 | ||
| C4-2B | Growth inhibition assay | 72 hrs | Growth inhibition of human C4-2B cells after 72 hrs by resazurin or MTT assay, GI50 = 4.15 μM. | 28156111 | ||
| DU145 | Growth inhibition assay | 72 hrs | Growth inhibition of human DU145 cells after 72 hrs by resazurin or MTT assay, GI50 = 5.792 μM. | 28156111 | ||
| MDA-MB-468 | Growth inhibition assay | 72 hrs | Growth inhibition of human MDA-MB-468 cells after 72 hrs by resazurin or MTT assay, GI50 = 5.96 μM. | 28156111 | ||
| BPH1 | Growth inhibition assay | 72 hrs | Growth inhibition of nontransformed human BPH1 cells after 72 hrs by resazurin or MTT assay, GI50 = 7.442 μM. | 28156111 | ||
| K562 | Cytotoxicity assay | 96 hrs | Cytotoxicity against human K562 cells after 96 hrs by Cell-Titer Blue assay, IC50 = 2 μM. | 24417566 | ||
| DU145 | Cytotoxicity assay | 96 hrs | Cytotoxicity against human DU145 cells after 96 hrs by Cell-Titer Blue assay, IC50 = 7.5 μM. | 24417566 | ||
| MDA-MB-231 | Cell cycle arrest assay | 0.5 to 1 uM | 24 hrs | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G1 phase at 0.5 to 1 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis | 24417566 | |
| MCF7 | Cell cycle arrest assay | 0.5 to 1 uM | 24 hrs | Cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 0.5 to 1 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis | 24417566 | |
| MDA-MB-231 | Function assay | 0.5 to 5 uM | 24 hrs | Inhibition of recombinant CDK4/cyclinD1 in human MDA-MB-231 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis | 24417566 | |
| MDA-MB-231 | Function assay | 0.5 to 5 uM | 24 hrs | Inhibition of recombinant CDK4/cyclinD1 in human MDA-MB-231 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis | 24417566 | |
| MCF7 | Function assay | 0.5 to 5 uM | 24 hrs | Inhibition of recombinant CDK4/cyclinD1 in human MCF7 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis | 24417566 | |
| MCF7 | Function assay | 0.5 to 5 uM | 24 hrs | Inhibition of recombinant CDK4/cyclinD1 in human MCF7 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis | 24417566 | |
| MV4-11 | Function assay | 12 to 24 hrs | Inhibition of CDK4/6 in human MV4-11 cells assessed as reduction in Rb phosphorylation at Ser780 at GI50 after 12 to 24 hrs by Western blot analysis | 28156111 | ||
| MV4-11 | Function assay | 12 to 24 hrs | Inhibition of CDK4/6 in human MV4-11 cells assessed as reduction in Rb phosphorylation at Ser780 at GI50 after 12 to 24 hrs by Western blot analysis | 28156111 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | |||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | |||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | |||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | |||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | |||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | |||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | |||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | |||
| Clicca per visualizzare più dati sperimentali sulle linee cellulari | ||||||
Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)
| Peso molecolare | 573.66 | Formula | C24H29N7O2.C2H6O4S |
Conservazione (Dalla data di ricezione) | |
|---|---|---|---|---|---|
| N. CAS | 827022-33-3 | Scarica SDF | Conservazione delle soluzioni stock |
|
|
| Sinonimi | PD0332991 Isethionate | Smiles | CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.C(CS(=O)(=O)O)O | ||
Solubilità (Solubility)
|
In vitro |
Water : 100 mg/mL
DMSO
: Insoluble
Ethanol : Insoluble |
Calcolatore di Molarità
Calcolatore di Diluizione
Calcolatore del Peso Molecolare
|
In vivo |
|||||
Calcolatore di formulazione in vivo (Soluzione chiara)
Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)
mg/kg
g
μL
Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Risultati del calcolo:
Concentrazione di lavoro: mg/ml;
Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.
Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.
Meccanismo d'azione (Mechanism of Action)
| Caratteristiche |
The 1st specific inhibitor for CDK4/6 to show promise in multiple cancers.
|
|---|---|
| Targets/IC50/Ki |
CDK4/CyclinD3
(Cell-free assay) 9 nM
CDK4/CyclinD1
(Cell-free assay) 11 nM
CDK6/CyclinD2
(Cell-free assay) 15 nM
|
| In vitro |
PD-0332991 (Palbociclib) Isethionate mostra una selettività assoluta per CDK4/6 con poca o nessuna attività contro altri CDK. PD-0332991 (Palbociclib) Isethionate è efficace nel ridurre la fosforilazione di Rb a Ser780 e Ser795 nelle cellule di carcinoma mammario MDA-MB-435 con un IC50 rispettivamente di 66 nM e 63 nM. PD-0332991 (Palbociclib) Isethionate è un potente inibitore della crescita cellulare e sopprime la replicazione del DNA impedendo alle cellule di entrare nella fase S. PD-0332991 (Palbociclib) Isethionate inibisce l'incorporazione di timidina nel DNA di carcinomi umani del seno Rb-positivi (come MDA-MB-435, MCF-7), del colon (H1299) e del polmone (Colo-205) così come nelle leucemie umane (CRRF-CEM e K562), con valori di IC50 che variano da 0,04 a 0,17 μM. PD-0332991 (Palbociclib) Isethionate aumenta significativamente la percentuale di MDA-MB-453 nel periodo G1. PD-0332991 (Palbociclib) Isethionate inibisce la fosforilazione di Rb nelle cellule di mieloma del midollo osseo primario CD138+ in ciclo, nelle cellule B primarie non trasformate e nelle linee cellulari MM1.S e CAG HMCL con IC50 rispettivamente di <0,1 μM, 0,05 μM e 60-70 nM. Il trattamento con PD-0332991 (Palbociclib) Isethionate induce anche l'arresto in G1 delle cellule di mieloma del midollo osseo primario CD138+ e delle cellule B primarie non trasformate. PD-0332991 (Palbociclib) Isethionate induce l'arresto in G1 in MM1.S con un IC50 di ~0,05 μM. PD-0332991 (Palbociclib) Isethionate inibisce preferenzialmente la proliferazione delle linee cellulari di cancro al seno umano luminali positive al recettore degli estrogeni (inclusi HER2-positivi). PD-0332991 (Palbociclib) Isethionate aumenta l'espressione genica di pRb e ciclina D1 e diminuisce l'espressione genica di CDKN2A (p16) nella maggior parte delle linee sensibili. PD-0332991 (Palbociclib) Isethionate migliora la sensibilità al tamoxifene nelle linee cellulari con resistenza condizionata al blocco degli ER.
|
| Saggio chinasico |
Saggi dell'attività CDK
|
|
I saggi CDK per le determinazioni della IC50 e la valutazione cinetica vengono eseguiti in piastre filtranti da 96 pozzetti. Tutti i complessi CDK-ciclina chinasi sono espressi in cellule di insetto tramite infezione da baculovirus e purificati. Il substrato per i saggi è un frammento (amminoacidi 792-928) di pRb fuso a GST (GST•RB-Cterm). Il volume di reazione totale è di 0,1 mL contenente una concentrazione finale di 20 mM Tris-HCl, pH 7,4, 50 mM NaCl, 1 mM ditiotreitolo, 10 mM MgCl2, 25 μM di ATP (per CDK4-ciclina D1, CDK6-ciclina D2 e CDK6-ciclina D3) contenente 0,25 μCi di [γ-32P]ATP, 20 ng di enzima, 1 μg di GST•RB-Cterm e appropriate diluizioni di inibitore. Tutti i componenti, eccetto il [γ-32P]ATP, vengono aggiunti ai pozzetti e posti su un miscelatore per piastre per 2 minuti. La reazione viene avviata aggiungendo il [γ-32P]ATP e incubata a 25 °C per 15 minuti. La reazione viene terminata con l'aggiunta di 0,1 mL di acido tricloroacetico al 20% e la piastra viene mantenuta a 4 °C per almeno 1 ora per consentire al substrato di precipitare. I pozzetti vengono quindi lavati cinque volte con 0,2 mL di acido tricloroacetico al 10% e l'incorporazione radioattiva viene determinata con un contatore di piastre β.
|
|
| In vivo |
PD-0332991 (Palbociclib) Isethionate (150 mg/kg) produce una rapida regressione degli xenotrapianti di carcinoma del colon Colo-205 e un corrispondente ritardo nella crescita tumorale. PD-0332991 (Palbociclib) Isethionate (150 mg/kg) induce una stasi tumorale completa e la morte cellulare nel carcinoma mammario MDA-MB-435. PD-0332991 (Palbociclib) Isethionate (150 mg/kg) induce inoltre una significativa regressione tumorale in topi portatori di xenotrapianti di glioblastoma SF-295 e in modelli di tumore mammario ZR-75-1 e prostatico PC-3 (soppressione completa della crescita tumorale). PD-0332991 (Palbociclib) Isethionate (150 mg/kg) sopprime la fosforilazione di Rb Ser780 nel carcinoma mammario MDA-MB-435 per l'intero periodo di 24 ore. PD-0332991 (Palbociclib) Isethionate (150 mg/kg) regola negativamente l'espressione di quattro geni regolati da E2F: CDC2, CCNE2, TK1 e TOP2A negli xenotrapianti di carcinoma Colo-205. PD-0332991 (Palbociclib) Isethionate inibisce anche rapidamente la crescita tumorale del mieloma.
|
Riferimenti |
|
Applicazioni (Applications)
| Metodi | Biomarcatori | Immagini | PMID |
|---|---|---|---|
| Western blot | RB1 (pT821) / RB1 (pS780) pAMPKα(T172) / AMPKα pULK1(S317) / ULK1 c-Jun / p-c-Jun / NFκB(p50) p38 / p-P38 / JNK / p-JNK |
|
30300583 |
| Growth inhibition assay | Cell viability IC50 |
|
28453226 |
| Immunofluorescence | γH2AX(Ser139) LC3B |
|
29669860 |
| ELISA | PGE2 |
|
26540629 |
Informazioni sullo studio clinico (Clinical Trial Information)
(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)
| Numero NCT | Reclutamento | Condizioni | Sponsor/Collaboratori | Data di inizio | Fasi |
|---|---|---|---|---|---|
| NCT05665361 | Recruiting | Advanced Clear Cell Renal Carcinoma (Ccrcc)|Papillary Renal Cell Carcinoma (Prcc) |
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
April 24 2024 | Phase 1|Phase 2 |
| NCT06307457 | Completed | Breast Cancer |
Pfizer |
March 11 2024 | -- |
| NCT05709158 | Not yet recruiting | Breast Cancer |
Pfizer |
March 1 2024 | -- |
| NCT05912933 | Not yet recruiting | Breast Cancer |
Pfizer |
March 1 2024 | -- |
Domande Frequenti (Frequently Asked Questions)
Domanda 1:
What is the best vehicle for it for in vitro and in vivo?
Risposta:
It can be used with water for vitro use and saline for vivo use.
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