solo per uso di ricerca
Tozasertib (VX-680) Aurora Kinase inibitore
N. Cat.S1048
Struttura chimica
Peso molecolare: 464.59
Vai a
Controllo Qualità
Lotto:
Purezza:
99.99%
99.99
| Target correlati | CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Casein Kinase |
|---|---|
| Altro Aurora Kinase Inibitori | Hesperadin Barasertib-HQPA (AZD2811) Alisertib (MLN8237) ZM 447439 MLN8054 Danusertib (PHA-739358) MK-5108 TCS7010 (Aurora A Inhibitor I) AMG-900 PHA-680632 |
Coltura cellulare, trattamento e concentrazione di lavoro
| Linee cellulari | Tipo di saggio | Concentrazione | Tempo di incubazione | Formulazione | Descrizione dellattività | PMID |
|---|---|---|---|---|---|---|
| BE-13 | Growth Inhibition Assay | IC50=0.00338 μM | SANGRER | |||
| RS4-11 | Growth Inhibition Assay | IC50=0.00404 μM | SANGRER | |||
| MFH-ino | Growth Inhibition Assay | IC50=0.0099 μM | SANGRER | |||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=0.01434 μM | SANGRER | |||
| 697 | Growth Inhibition Assay | IC50=0.02471 μM | SANGRER | |||
| NALM-6 | Growth Inhibition Assay | IC50=0.02552 μM | SANGRER | |||
| ES8 | Growth Inhibition Assay | IC50=0.04613 μM | SANGRER | |||
| HUTU-80 | Growth Inhibition Assay | IC50=0.05299 μM | SANGRER | |||
| MV-4-11 | Growth Inhibition Assay | IC50=0.07782 μM | SANGRER | |||
| MONO-MAC-6 | Growth Inhibition Assay | IC50=0.07879 μM | SANGRER | |||
| LC-2-ad | Growth Inhibition Assay | IC50=0.08789 μM | SANGRER | |||
| BL-41 | Growth Inhibition Assay | IC50=0.10445 μM | SANGRER | |||
| A4-Fuk | Growth Inhibition Assay | IC50=0.11563 μM | SANGRER | |||
| SW954 | Growth Inhibition Assay | IC50=0.12229 μM | SANGRER | |||
| BV-173 | Growth Inhibition Assay | IC50=0.12641 μM | SANGRER | |||
| TE-11 | Growth Inhibition Assay | IC50=0.14982 μM | SANGRER | |||
| SK-UT-1 | Growth Inhibition Assay | IC50=0.15965 μM | SANGRER | |||
| SIG-M5 | Growth Inhibition Assay | IC50=0.16707 μM | SANGRER | |||
| OCUB-M | Growth Inhibition Assay | IC50=0.16983 μM | SANGRER | |||
| K052 | Growth Inhibition Assay | IC50=0.1948 μM | SANGRER | |||
| VA-ES-BJ | Growth Inhibition Assay | IC50=0.20086 μM | SANGRER | |||
| SW982 | Growth Inhibition Assay | IC50=0.2138 μM | SANGRER | |||
| LB647-SCLC | Growth Inhibition Assay | IC50=0.21523 μM | SANGRER | |||
| PSN1 | Growth Inhibition Assay | IC50=0.22026 μM | SANGRER | |||
| BB30-HNC | Growth Inhibition Assay | IC50=0.22591 μM | SANGRER | |||
| ST486 | Growth Inhibition Assay | IC50=0.23087 μM | SANGRER | |||
| MOLT-4 | Growth Inhibition Assay | IC50=0.23337 μM | SANGRER | |||
| EW-16 | Growth Inhibition Assay | IC50=0.23768 μM | SANGRER | |||
| KS-1 | Growth Inhibition Assay | IC50=0.23785 μM | SANGRER | |||
| SR | Growth Inhibition Assay | IC50=0.24564 μM | SANGRER | |||
| KM12 | Growth Inhibition Assay | IC50=0.2636 μM | SANGRER | |||
| EM-2 | Growth Inhibition Assay | IC50=0.26641 μM | SANGRER | |||
| MEG-01 | Growth Inhibition Assay | IC50=0.27849 μM | SANGRER | |||
| NB13 | Growth Inhibition Assay | IC50=0.27984 μM | SANGRER | |||
| RKO | Growth Inhibition Assay | IC50=0.30813 μM | SANGRER | |||
| CESS | Growth Inhibition Assay | IC50=0.31328 μM | SANGRER | |||
| EoL-1-cell | Growth Inhibition Assay | IC50=0.33459 μM | SANGRER | |||
| DOHH-2 | Growth Inhibition Assay | IC50=0.33781 μM | SANGRER | |||
| A388 | Growth Inhibition Assay | IC50=0.34086 μM | SANGRER | |||
| LAMA-84 | Growth Inhibition Assay | IC50=0.35178 μM | SANGRER | |||
| IMR-5 | Growth Inhibition Assay | IC50=0.3554 μM | SANGRER | |||
| KARPAS-422 | Growth Inhibition Assay | IC50=0.37272 μM | SANGRER | |||
| MRK-nu-1 | Growth Inhibition Assay | IC50=0.3813 μM | SANGRER | |||
| BL-70 | Growth Inhibition Assay | IC50=0.38974 μM | SANGRER | |||
| LXF-289 | Growth Inhibition Assay | IC50=0.40406 μM | SANGRER | |||
| RL95-2 | Growth Inhibition Assay | IC50=0.40567 μM | SANGRER | |||
| QIMR-WIL | Growth Inhibition Assay | IC50=0.42676 μM | SANGRER | |||
| K-562 | Growth Inhibition Assay | IC50=0.43472 μM | SANGRER | |||
| NCI-H510A | Growth Inhibition Assay | IC50=0.43823 μM | SANGRER | |||
| NCI-H524 | Growth Inhibition Assay | IC50=0.51147 μM | SANGRER | |||
| KE-37 | Growth Inhibition Assay | IC50=0.52102 μM | SANGRER | |||
| KP-N-YS | Growth Inhibition Assay | IC50=0.54392 μM | SANGRER | |||
| LS-411N | Growth Inhibition Assay | IC50=0.57752 μM | SANGRER | |||
| CTV-1 | Growth Inhibition Assay | IC50=0.58773 μM | SANGRER | |||
| NCI-SNU-16 | Growth Inhibition Assay | IC50=0.63571 μM | SANGRER | |||
| HT-144 | Growth Inhibition Assay | IC50=0.63798 μM | SANGRER | |||
| NCI-H187 | Growth Inhibition Assay | IC50=0.6413 μM | SANGRER | |||
| OCI-AML2 | Growth Inhibition Assay | IC50=0.64403 μM | SANGRER | |||
| CCRF-CEM | Growth Inhibition Assay | IC50=0.65346 μM | SANGRER | |||
| ONS-76 | Growth Inhibition Assay | IC50=0.66458 μM | SANGRER | |||
| IST-SL2 | Growth Inhibition Assay | IC50=0.71982 μM | SANGRER | |||
| NB6 | Growth Inhibition Assay | IC50=0.77254 μM | SANGRER | |||
| SK-PN-DW | Growth Inhibition Assay | IC50=0.7914 μM | SANGRER | |||
| HCC1599 | Growth Inhibition Assay | IC50=0.80874 μM | SANGRER | |||
| MC116 | Growth Inhibition Assay | IC50=0.85011 μM | SANGRER | |||
| TE-15 | Growth Inhibition Assay | IC50=0.85098 μM | SANGRER | |||
| HOP-62 | Growth Inhibition Assay | IC50=0.86329 μM | SANGRER | |||
| TGBC24TKB | Growth Inhibition Assay | IC50=0.86385 μM | SANGRER | |||
| HCE-4 | Growth Inhibition Assay | IC50=0.88063 μM | SANGRER | |||
| ALL-PO | Growth Inhibition Assay | IC50=0.88175 μM | SANGRER | |||
| KGN | Growth Inhibition Assay | IC50=0.89995 μM | SANGRER | |||
| ML-2 | Growth Inhibition Assay | IC50=0.90259 μM | SANGRER | |||
| ES4 | Growth Inhibition Assay | IC50=0.91128 μM | SANGRER | |||
| SF126 | Growth Inhibition Assay | IC50=0.94819 μM | SANGRER | |||
| SK-N-DZ | Growth Inhibition Assay | IC50=0.96189 μM | SANGRER | |||
| HCC1187 | Growth Inhibition Assay | IC50=1.00505 μM | SANGRER | |||
| DU-4475 | Growth Inhibition Assay | IC50=1.01756 μM | SANGRER | |||
| NKM-1 | Growth Inhibition Assay | IC50=1.02775 μM | SANGRER | |||
| HL-60 | Growth Inhibition Assay | IC50=1.06574 μM | SANGRER | |||
| SBC-1 | Growth Inhibition Assay | IC50=1.12542 μM | SANGRER | |||
| TE-10 | Growth Inhibition Assay | IC50=1.12946 μM | SANGRER | |||
| ETK-1 | Growth Inhibition Assay | IC50=1.13613 μM | SANGRER | |||
| HAL-01 | Growth Inhibition Assay | IC50=1.16709 μM | SANGRER | |||
| BB65-RCC | Growth Inhibition Assay | IC50=1.18005 μM | SANGRER | |||
| EW-1 | Growth Inhibition Assay | IC50=1.18562 μM | SANGRER | |||
| SK-NEP-1 | Growth Inhibition Assay | IC50=1.21111 μM | SANGRER | |||
| SK-LMS-1 | Growth Inhibition Assay | IC50=1.22212 μM | SANGRER | |||
| DEL | Growth Inhibition Assay | IC50=1.25643 μM | SANGRER | |||
| GT3TKB | Growth Inhibition Assay | IC50=1.28057 μM | SANGRER | |||
| MOLT-16 | Growth Inhibition Assay | IC50=1.35405 μM | SANGRER | |||
| CMK | Growth Inhibition Assay | IC50=1.42117 μM | SANGRER | |||
| NB5 | Growth Inhibition Assay | IC50=1.64229 μM | SANGRER | |||
| NCI-H1963 | Growth Inhibition Assay | IC50=1.70583 μM | SANGRER | |||
| KURAMOCHI | Growth Inhibition Assay | IC50=1.78911 μM | SANGRER | |||
| TE-8 | Growth Inhibition Assay | IC50=1.80368 μM | SANGRER | |||
| NCI-H1304 | Growth Inhibition Assay | IC50=1.83073 μM | SANGRER | |||
| A101D | Growth Inhibition Assay | IC50=1.87395 μM | SANGRER | |||
| SCLC-21H | Growth Inhibition Assay | IC50=1.97057 μM | SANGRER | |||
| GB-1 | Growth Inhibition Assay | IC50=2.01647 μM | SANGRER | |||
| KARPAS-45 | Growth Inhibition Assay | IC50=2.02654 μM | SANGRER | |||
| ATN-1 | Growth Inhibition Assay | IC50=2.02858 μM | SANGRER | |||
| NCI-H720 | Growth Inhibition Assay | IC50=2.06244 μM | SANGRER | |||
| RPMI-6666 | Growth Inhibition Assay | IC50=2.16207 μM | SANGRER | |||
| NB17 | Growth Inhibition Assay | IC50=2.2927 μM | SANGRER | |||
| IST-SL1 | Growth Inhibition Assay | IC50=2.29765 μM | SANGRER | |||
| SH-4 | Growth Inhibition Assay | IC50=2.32469 μM | SANGRER | |||
| K5 | Growth Inhibition Assay | IC50=2.40319 μM | SANGRER | |||
| OVCAR-4 | Growth Inhibition Assay | IC50=2.4613 μM | SANGRER | |||
| ACN | Growth Inhibition Assay | IC50=2.50213 μM | SANGRER | |||
| TGW | Growth Inhibition Assay | IC50=2.65832 μM | SANGRER | |||
| NCI-H2107 | Growth Inhibition Assay | IC50=2.83711 μM | SANGRER | |||
| NCI-H82 | Growth Inhibition Assay | IC50=2.83838 μM | SANGRER | |||
| SK-N-FI | Growth Inhibition Assay | IC50=2.86868 μM | SANGRER | |||
| LB1047-RCC | Growth Inhibition Assay | IC50=2.88126 μM | SANGRER | |||
| LU-134-A | Growth Inhibition Assay | IC50=2.8926 μM | SANGRER | |||
| NCI-H209 | Growth Inhibition Assay | IC50=2.91253 μM | SANGRER | |||
| NOMO-1 | Growth Inhibition Assay | IC50=3.02274 μM | SANGRER | |||
| RH-1 | Growth Inhibition Assay | IC50=3.17291 μM | SANGRER | |||
| LOUCY | Growth Inhibition Assay | IC50=3.18693 μM | SANGRER | |||
| TE-9 | Growth Inhibition Assay | IC50=3.26736 μM | SANGRER | |||
| PF-382 | Growth Inhibition Assay | IC50=3.35778 μM | SANGRER | |||
| RPMI-8402 | Growth Inhibition Assay | IC50=3.58603 μM | SANGRER | |||
| HEL | Growth Inhibition Assay | IC50=3.632 μM | SANGRER | |||
| NOS-1 | Growth Inhibition Assay | IC50=3.84754 μM | SANGRER | |||
| ES1 | Growth Inhibition Assay | IC50=3.92293 μM | SANGRER | |||
| NCI-H2171 | Growth Inhibition Assay | IC50=3.92423 μM | SANGRER | |||
| NCI-H747 | Growth Inhibition Assay | IC50=3.94221 μM | SANGRER | |||
| MHH-NB-11 | Growth Inhibition Assay | IC50=3.95312 μM | SANGRER | |||
| MZ1-PC | Growth Inhibition Assay | IC50=3.9924 μM | SANGRER | |||
| MMAC-SF | Growth Inhibition Assay | IC50=4.02467 μM | SANGRER | |||
| NMC-G1 | Growth Inhibition Assay | IC50=4.22723 μM | SANGRER | |||
| SW872 | Growth Inhibition Assay | IC50=4.3434 μM | SANGRER | |||
| TE-12 | Growth Inhibition Assay | IC50=4.56394 μM | SANGRER | |||
| LU-139 | Growth Inhibition Assay | IC50=4.61835 μM | SANGRER | |||
| HC-1 | Growth Inhibition Assay | IC50=4.69494 μM | SANGRER | |||
| COR-L279 | Growth Inhibition Assay | IC50=4.75891 μM | SANGRER | |||
| SF268 | Growth Inhibition Assay | IC50=4.79916 μM | SANGRER | |||
| MC-CAR | Growth Inhibition Assay | IC50=5.06757 μM | SANGRER | |||
| TK10 | Growth Inhibition Assay | IC50=5.35469 μM | SANGRER | |||
| TE-1 | Growth Inhibition Assay | IC50=5.49004 μM | SANGRER | |||
| NCI-H2126 | Growth Inhibition Assay | IC50=5.64574 μM | SANGRER | |||
| Daudi | Growth Inhibition Assay | IC50=5.6912 μM | SANGRER | |||
| NCI-H1648 | Growth Inhibition Assay | IC50=5.81454 μM | SANGRER | |||
| OS-RC-2 | Growth Inhibition Assay | IC50=5.98597 μM | SANGRER | |||
| DJM-1 | Growth Inhibition Assay | IC50=6.34666 μM | SANGRER | |||
| LS-1034 | Growth Inhibition Assay | IC50=6.7566 μM | SANGRER | |||
| NCI-H1581 | Growth Inhibition Assay | IC50=6.78405 μM | SANGRER | |||
| UACC-257 | Growth Inhibition Assay | IC50=7.04512 μM | SANGRER | |||
| KM-H2 | Growth Inhibition Assay | IC50=7.18457 μM | SANGRER | |||
| NCI-H1436 | Growth Inhibition Assay | IC50=7.69932 μM | SANGRER | |||
| IA-LM | Growth Inhibition Assay | IC50=7.859 μM | SANGRER | |||
| NCI-H526 | Growth Inhibition Assay | IC50=8.25637 μM | SANGRER | |||
| GCIY | Growth Inhibition Assay | IC50=8.36965 μM | SANGRER | |||
| CP67-MEL | Growth Inhibition Assay | IC50=8.5326 μM | SANGRER | |||
| KALS-1 | Growth Inhibition Assay | IC50=8.83851 μM | SANGRER | |||
| NCI-H1770 | Growth Inhibition Assay | IC50=8.90265 μM | SANGRER | |||
| 8-MG-BA | Growth Inhibition Assay | IC50=9.32844 μM | SANGRER | |||
| KY821 | Growth Inhibition Assay | IC50=9.77484 μM | SANGRER | |||
| SNB75 | Growth Inhibition Assay | IC50=10.076 μM | SANGRER | |||
| NCCIT | Growth Inhibition Assay | IC50=11.0582 μM | SANGRER | |||
| SJSA-1 | Growth Inhibition Assay | IC50=11.2891 μM | SANGRER | |||
| LB373-MEL-D | Growth Inhibition Assay | IC50=11.3827 μM | SANGRER | |||
| TALL-1 | Growth Inhibition Assay | IC50=11.4058 μM | SANGRER | |||
| NB69 | Growth Inhibition Assay | IC50=11.7705 μM | SANGRER | |||
| NCI-H1355 | Growth Inhibition Assay | IC50=11.9426 μM | SANGRER | |||
| DMS-153 | Growth Inhibition Assay | IC50=12.0426 μM | SANGRER | |||
| OPM-2 | Growth Inhibition Assay | IC50=12.1596 μM | SANGRER | |||
| NB1 | Growth Inhibition Assay | IC50=12.29 μM | SANGRER | |||
| A3-KAW | Growth Inhibition Assay | IC50=12.3236 μM | SANGRER | |||
| NCI-H1882 | Growth Inhibition Assay | IC50=12.4066 μM | SANGRER | |||
| KG-1 | Growth Inhibition Assay | IC50=12.6545 μM | SANGRER | |||
| LC4-1 | Growth Inhibition Assay | IC50=12.7706 μM | SANGRER | |||
| HCE-T | Growth Inhibition Assay | IC50=13.0049 μM | SANGRER | |||
| NEC8 | Growth Inhibition Assay | IC50=13.1038 μM | SANGRER | |||
| IST-MEL1 | Growth Inhibition Assay | IC50=13.5788 μM | SANGRER | |||
| EW-3 | Growth Inhibition Assay | IC50=13.7402 μM | SANGRER | |||
| CTB-1 | Growth Inhibition Assay | IC50=14.0329 μM | SANGRER | |||
| LS-123 | Growth Inhibition Assay | IC50=14.1588 μM | SANGRER | |||
| NCI-H1417 | Growth Inhibition Assay | IC50=14.3052 μM | SANGRER | |||
| MZ7-mel | Growth Inhibition Assay | IC50=14.4433 μM | SANGRER | |||
| JiyoyeP-2003 | Growth Inhibition Assay | IC50=15.6326 μM | SANGRER | |||
| ES6 | Growth Inhibition Assay | IC50=16.2361 μM | SANGRER | |||
| HH | Growth Inhibition Assay | IC50=17.1963 μM | SANGRER | |||
| SF539 | Growth Inhibition Assay | IC50=17.9922 μM | SANGRER | |||
| Calu-6 | Growth Inhibition Assay | IC50=19.239 μM | SANGRER | |||
| SK-MM-2 | Growth Inhibition Assay | IC50=19.555 μM | SANGRER | |||
| IST-MES1 | Growth Inhibition Assay | IC50=19.6663 μM | SANGRER | |||
| GI-ME-N | Growth Inhibition Assay | IC50=19.8227 μM | SANGRER | |||
| CAL-148 | Growth Inhibition Assay | IC50=20.9934 μM | SANGRER | |||
| EVSA-T | Growth Inhibition Assay | IC50=21.1499 μM | SANGRER | |||
| LP-1 | Growth Inhibition Assay | IC50=21.3432 μM | SANGRER | |||
| BOKU | Growth Inhibition Assay | IC50=21.4533 μM | SANGRER | |||
| KLE | Growth Inhibition Assay | IC50=22.1903 μM | SANGRER | |||
| LB831-BLC | Growth Inhibition Assay | IC50=25.1526 μM | SANGRER | |||
| NCI-H889 | Growth Inhibition Assay | IC50=25.1931 μM | SANGRER | |||
| REH | Growth Inhibition Assay | IC50=25.4671 μM | SANGRER | |||
| KP-N-RT-BM-1 | Growth Inhibition Assay | IC50=25.4752 μM | SANGRER | |||
| MPP-89 | Growth Inhibition Assay | IC50=25.5314 μM | SANGRER | |||
| no-11 | Growth Inhibition Assay | IC50=25.747 μM | SANGRER | |||
| NCI-H748 | Growth Inhibition Assay | IC50=25.7627 μM | SANGRER | |||
| LB2518-MEL | Growth Inhibition Assay | IC50=27.1773 μM | SANGRER | |||
| TGBC1TKB | Growth Inhibition Assay | IC50=27.5585 μM | SANGRER | |||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=28.0734 μM | SANGRER | |||
| MZ2-MEL | Growth Inhibition Assay | IC50=28.6143 μM | SANGRER | |||
| U-266 | Growth Inhibition Assay | IC50=28.6366 μM | SANGRER | |||
| SNU-C1 | Growth Inhibition Assay | IC50=28.943 μM | SANGRER | |||
| SW962 | Growth Inhibition Assay | IC50=30.2747 μM | SANGRER | |||
| Raji | Growth Inhibition Assay | IC50=30.5592 μM | SANGRER | |||
| KNS-42 | Growth Inhibition Assay | IC50=30.8956 μM | SANGRER | |||
| LB996-RCC | Growth Inhibition Assay | IC50=31.1702 μM | SANGRER | |||
| CHP-126 | Growth Inhibition Assay | IC50=31.1984 μM | SANGRER | |||
| RXF393 | Growth Inhibition Assay | IC50=32.497 μM | SANGRER | |||
| COLO-684 | Growth Inhibition Assay | IC50=32.6438 μM | SANGRER | |||
| A704 | Growth Inhibition Assay | IC50=33.5538 μM | SANGRER | |||
| A253 | Growth Inhibition Assay | IC50=33.5852 μM | SANGRER | |||
| KNS-81-FD | Growth Inhibition Assay | IC50=34.5456 μM | SANGRER | |||
| TE-441-T | Growth Inhibition Assay | IC50=34.6371 μM | SANGRER | |||
| HCC2157 | Growth Inhibition Assay | IC50=35.4619 μM | SANGRER | |||
| ES3 | Growth Inhibition Assay | IC50=36.675 μM | SANGRER | |||
| NCI-H1155 | Growth Inhibition Assay | IC50=37.815 μM | SANGRER | |||
| SNU-C2B | Growth Inhibition Assay | IC50=38.1654 μM | SANGRER | |||
| JAR | Growth Inhibition Assay | IC50=38.2449 μM | SANGRER | |||
| GDM-1 | Growth Inhibition Assay | IC50=38.9116 μM | SANGRER | |||
| KU812 | Growth Inhibition Assay | IC50=41.507 μM | SANGRER | |||
| BC-1 | Growth Inhibition Assay | IC50=42.6731 μM | SANGRER | |||
| GI-1 | Growth Inhibition Assay | IC50=42.9192 μM | SANGRER | |||
| NCI-H1694 | Growth Inhibition Assay | IC50=44.9472 μM | SANGRER | |||
| DG-75 | Growth Inhibition Assay | IC50=45.1577 μM | SANGRER | |||
| COR-L88 | Growth Inhibition Assay | IC50=45.2778 μM | SANGRER | |||
| LS-513 | Growth Inhibition Assay | IC50=45.9156 μM | SANGRER | |||
| HD-MY-Z | Growth Inhibition Assay | IC50=46.4612 μM | SANGRER | |||
| L-363 | Growth Inhibition Assay | IC50=46.881 μM | SANGRER | |||
| TE-6 | Growth Inhibition Assay | IC50=48.446 μM | SANGRER | |||
| NCI-H345 | Growth Inhibition Assay | IC50=48.468 μM | SANGRER | |||
| TE-5 | Growth Inhibition Assay | IC50=49.7118 μM | SANGRER | |||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells, IC50=0.048μM | 18630890 | |||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells, IC50=0.053μM | 18630890 | |||
| HT29 | Antiproliferative assay | Antiproliferative activity against human HT29 cells, IC50=0.15μM | 18630890 | |||
| HCT | Function assay | Inhibition of Aurora A in human HCT cells assessed as loss of autophosphorylation of Aurora A, IC50=0.31μM | 18630890 | |||
| HCT | Function assay | Inhibition of Aurora A assessed as separation of centrosomes in human HCT cells, IC50=0.31μM | 18630890 | |||
| HCT | Function assay | Inhibition of Aurora B assessed as loss of phospho histone H3 in human HCT cells, IC50=0.31μM | 18630890 | |||
| H29 | Function assay | Inhibition of Aurora B assessed as loss of phospho histone H3 in human H29 cells, IC50=0.74μM | 18630890 | |||
| HCT116 | Cytotoxicity assay | 10 to 14 days | Cytotoxicity against human HCT116 cells assessed as number of colonies after 10 to 14 days by colony forming assay, IC50=0.024μM | 19143567 | ||
| HCT116 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HCT116 cells assessed as distinct polyploidy phenotype after 72 hrs, Activity=0.03μM | 19143567 | ||
| COLO205 | Antiproliferative assay | Antiproliferative activity against human COLO205 cells by [3H]thymidine uptake assay, IC50=0.019μM | 19447622 | |||
| HCT116 | Cytotoxicity assay | Cytotoxicity against human HCT116 cells by MTS assay, IC50=0.12μM | 20550212 | |||
| HeLa | Function assay | Inhibition of phosphotransferase activity of recombinant aurora A expressed in HeLa cells, Ki=0.002μM | 20573509 | |||
| BA/F3 | Antiproliferative assay | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant, IC50=0.03μM | 20604564 | |||
| BA/F3 | Function assay | Inhibition of Bcr-Abl T315I mutant autophosphorylation in mouse BA/F3 cells, IC50=5μM | 20604564 | |||
| insect | Function assay | Inhibition of human recombinant His-tagged Aurora A kinase expressed in insect cells, IC50=0.0007μM | 21194953 | |||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells, IC50=0.028μM | 21802948 | |||
| HCT116 | Function assay | Inhibition of Aurora B kinase assessed as reduction in histone H3 phosphorylation in human HCT116 cells, IC50=0.055μM | 21802948 | |||
| HCT116 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay, IC50=0.3μM | 22572580 | ||
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=0.38μM | 22572580 | ||
| sf9 | Function assay | 15 mins | Inhibition of GST-tagged Aurora kinase A catalytic domain (123 to 401 amino acids) (unknown origin) expressed in sf9 cells using tetra(LRRWSLG) as substrate preincubated for 15 mins prior to substrate addition measured after 90 mins by luminescence assay, IC50=0.02μM | 23808327 | ||
| HCT116 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human HCT116 cells after 96 hrs by MTS assay, EC50=0.12μM | 23808327 | ||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells, IC50=0.12μM | 23808327 | |||
| HCT116 | Antitumor assay | 50 mg/kg | 5 days | Antitumor activity against human HCT116 cells xenografted in athymic nu/nu mouse assessed as reduction in tumor size at 50 mg/kg, iv qd for 5 days per week for 2 weeks measured twice a week | 23808327 | |
| HeLa | Function assay | 10 to 1000 nM | 48 hrs | Inhibition of Aurora kinase B in human HeLa cells assessed as delay in mitotic arrest by accumulation of multinucleated cells with 4N/8N DNA content at 10 to 1000 nM after 48 hrs by propidium iodide staining-based FACS flow cytometric analysis | 23808327 | |
| MOLT4 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MOLT4 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.0212μM | 24681066 | ||
| U937 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.036μM | 24681066 | ||
| HL60 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HL60 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.0382μM | 24681066 | ||
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.0791μM | 24681066 | ||
| MDA-MB-231 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.127μM | 24681066 | ||
| A431 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A431 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.24μM | 24681066 | ||
| DU145 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human DU145 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.4μM | 24681066 | ||
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=1.3μM | 24681066 | ||
| HeLa | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HeLa cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=2.93μM | 24681066 | ||
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=3.05μM | 24681066 | ||
| PANC1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human PANC1 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=4.13μM | 24681066 | ||
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=4.32μM | 24681066 | ||
| PC3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human PC3 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=5.81μM | 24681066 | ||
| SKBR3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SKBR3 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=9.99μM | 24681066 | ||
| NCI-N87 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-N87 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=11.6μM | 24681066 | ||
| HepG2 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, TC50=3.3μM | 24910766 | ||
| HeLa | Function assay | 12 hrs | Inhibition of Aurora A in human HeLa cells after 12 hrs by ELISA method, IC50=0.261μM | 25812967 | ||
| HeLa | Function assay | 12 hrs | Inhibition of Aurora B in human HeLa cells after 12 hrs by ELISA method, IC50=0.453μM | 25812967 | ||
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50=19.4μM | 25812967 | ||
| HeLa | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50=27.3μM | 25812967 | ||
| HCT8 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCT8 cells after 48 hrs by MTT assay, IC50=44.6μM | 25812967 | ||
| Hela | Function assay | Inhibition of recombinant Aurora A kinase derived from human Hela cells using kemptide as substrate in presence of [c-32P]ATP, Ki=0.002μM | 27884697 | |||
| NCI-H23 | Antiproliferative assay | Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant at | 28038940 | |||
| NCI-H358 | Antiproliferative assay | Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant at | 28038940 | |||
| U937 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human U937 cells after 48 hrs by CCK8 assay, IC50=0.036μM | 29358147 | ||
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay, IC50=0.079μM | 29358147 | ||
| MDA-MB-231 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by CCK8 assay, IC50=0.127μM | 29358147 | ||
| A431 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A431 cells after 48 hrs by CCK8 assay, IC50=0.24μM | 29358147 | ||
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by CCK8 assay, IC50=1.3μM | 29358147 | ||
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells after 48 hrs by CCK8 assay, IC50=2.93μM | 29358147 | ||
| HCT116 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HCT116 cells after 48 hrs by CCK8 assay, IC50=4.32μM | 29358147 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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 | |||
| 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 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | |||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | |||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 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 | |||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | |||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | |||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 29435139 | |||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | |||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | |||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 29435139 | |||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | |||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 29435139 | |||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | |||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | |||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 29435139 | |||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 29435139 | |||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | |||
| L929sA | Function assay | 24 hrs | Inhibition of Aurk mouse L929sA cells transfected with human Fas assessed as reduction in cell growth after 24 hrs in presence of TNF by Hoechst 33342 staining-based microscopic assay, IC50=0.97μM | 29437386 | ||
| L929sA | Function assay | 0.5 hrs | Inhibition of RIPK1 in mouse L929sA cells transfected with human Fas assessed as inhibition in TNF-induced necroptosis pretreated for 0.5 hrs followed by TNF and zVAD.fmk addition measured after 3 hrs by Hoechst 33342/propidium iodide staining-based assay, IC50=0.98μM | 29437386 | ||
| L929sA | Function assay | 24 hrs | Inhibition of RIPK1 in mouse L929sA cells transfected with human Fas assessed as inhibition in TNF-induced necroptosis pretreated for 24 hrs followed by TNF and zVAD.fmk addition measured after 3 hrs by Hoechst 33342/propidium iodide staining-based assay, IC50=1.02μM | 29437386 | ||
| L929sA | Function assay | 24 hrs | Inhibition of Aurk mouse L929sA cells transfected with human Fas assessed as increase in nuclear area after 24 hrs in presence of TNF by Hoechst 33342 staining-based microscopic assay, IC50=1.06μM | 29437386 | ||
| HCT116 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=0.45μM | 30143423 | ||
| HCT15 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCT15 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=1.23μM | 30143423 | ||
| HCT116 | Function assay | 100 nM | 24 hrs | Inhibition of cytokinesis in human HCT116 cells at 100 nM after 24 hrs by propidium iodide/RNase staining-based flow cytometric analysis | 30143423 | |
| HCT116 | Function assay | 1 uM | 24 hrs | Inhibition of cytokinesis in human HCT116 cells at 1 uM after 24 hrs by propidium iodide/RNase staining-based flow cytometric analysis | 30143423 | |
| HCT116 | Function assay | 1 uM | 3 hrs | Inhibition of Aurora B in human HCT116 cells assessed as reduction in histone H3 phosphorylation at Ser10 residue up to 1 uM after 3 hrs by Western blot analysis | 30143423 | |
| HCT116 | Function assay | 3 hrs | Inhibition of Aurora A phosphorylation at Thr288 residue in human HCT116 cells up to 1 uM after 3 hrs by Western blot analysis | 30143423 | ||
| HCT116 | Function assay | 3 hrs | Inhibition of Aurora B phosphorylation at Thr232 residue in human HCT116 cells up to 1 uM after 3 hrs by Western blot method | 30143423 | ||
| Sf9 | Function assay | Inhibition of GST-tagged AURORA A (unknown origin) expressed in baculovirus infected Sf9 cells using MBP as substrate, IC50=0.023μM | 30234987 | |||
| HeLa | Function assay | 12 hrs | Inhibition of Aurora A phosphorylation at Thr288 residue in human HeLa cells after 12 hrs by ELISA, IC50=0.013μM | 30502115 | ||
| HeLa | Function assay | 12 hrs | Inhibition of Aurora B phosphorylation at Thr232 residue in human HeLa cells after 12 hrs by ELISA, IC50=0.148μM | 30502115 | ||
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, GI50=35.8μM | 30502115 | ||
| LoVo | Antiproliferative assay | 48 hrs | Antiproliferative activity against human LoVo cells after 48 hrs by MTT assay, GI50=45.3μM | 30502115 | ||
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, GI50=46.2μM | 30502115 | ||
| HeLa | Cell cycle assay | 5 uM | 12 hrs | Cell cycle arrest in human HeLa cells assessed as decrease in cyclin B1 protein expression at 5 uM after 12 hrs by Western blot analysis | 30502115 | |
| HeLa | Cell cycle assay | 5 uM | 12 hrs | Cell cycle arrest in human HeLa cells assessed as decrease in cdc2 protein expression at 5 uM after 12 hrs by Western blot analysis | 30502115 | |
| HeLa | Function assay | 5 uM | 12 hrs | Inhibition of Aurora A phosphorylation at Thr288 residue in human HeLa cells at 5 uM after 12 hrs by Western blot analysis | 30502115 | |
| HeLa | Function assay | 5 uM | 12 hrs | Inhibition of Aurora B phosphorylation at Thr232 residue in human HeLa cells at 5 uM after 12 hrs by Western blot analysis | 30502115 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50=35.8μM | 30728112 | ||
| LoVo | Antiproliferative assay | 48 hrs | Antiproliferative activity against human LoVo cells after 48 hrs by MTT assay, IC50=45.3μM | 30728112 | ||
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, IC50=46.2μM | 30728112 | ||
| Clicca per visualizzare più dati sperimentali sulle linee cellulari | ||||||
Informazioni chimiche, conservazione e stabilità
| Peso molecolare | 464.59 | Formula | C23H28N8OS |
Conservazione (Dalla data di ricezione) | |
|---|---|---|---|---|---|
| N. CAS | 639089-54-6 | Scarica SDF | Conservazione delle soluzioni stock |
|
|
| Sinonimi | MK-0457 | Smiles | CC1=CC(=NN1)NC2=CC(=NC(=N2)SC3=CC=C(C=C3)NC(=O)C4CC4)N5CCN(CC5)C | ||
Solubilità
|
In vitro |
DMSO
: 93 mg/mL
(200.17 mM)
Ethanol : 40 mg/mL Water : 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 lesperimento)
mg/kg
g
μL
Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè 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, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.
Meccanismo dazione
| Targets/IC50/Ki |
Aurora A
(Cell-free assay) 0.6 nM(Ki app)
Aurora C
(Cell-free assay) 4.6 nM(Ki app)
Aurora B
(Cell-free assay) 18 nM(Ki app)
FLT3
(Cell-free assay) 30 nM(Ki)
Bcr-Abl
(Cell-free assay) 30 nM(Ki)
|
|---|---|
| In vitro |
Nonostante il suo profilo multi-chinasico, Tozasertib (VX-680) induce una citotossicità simile con un IC50 di circa 300 nM e mostra un fenotipo inibitorio simile a AUR B di arresto G2/M, endoreduplicazione e apoptosi nelle cellule BaF3 trasfettate con chinasi ABL o FLT-3 (mutante e wild type). Questo composto previene la proliferazione di CAL-62 in modo tempo-dipendente. Il trattamento per 14 giorni diminuisce significativamente il numero e la dimensione delle colonie di circa il 70% nel 8305C e del 90% nel CAL-62, 8505C e BHT-101. Il trattamento delle diverse cellule ATC con esso inibisce la proliferazione con un IC50 tra 25 e 150 nM. Compromette significativamente la capacità delle diverse linee cellulari di formare colonie in agar molle. L'analisi dell'attività della caspasi-3 indica che VX-680 induce apoptosi nelle diverse linee cellulari. Le cellule CAL-62 esposte per 12 ore al composto hanno mostrato un accumulo di cellule con un contenuto di DNA ≥4N. L'analisi time-lapse dimostra che le cellule CAL-62 trattate escono dalla metafase senza dividersi. Inoltre, la fosforilazione dell'istone H3 è abrogata in seguito al suo trattamento. Ha una significativa attività inibitoria contro BCR-Abl portante la mutazione T315I in campioni derivati da pazienti.
|
| Saggio chinasico |
Saggi di inibizione della chinasi
|
|
Il consumo di ATP è accoppiato, tramite la coppia enzimatica piruvato chinasi/lattato deidrogenasi, all'ossidazione del NADH, che può essere monitorata attraverso la diminuzione dell'assorbimento a 340 nm. Le reazioni contengono 100 mM Tris (pH 8), 10 mM MgCl2, 2,2 mM ATP, 1 mM fosfoenolpiruvato, 0,6 mg/mL NADH, 75 unità/mL piruvato chinasi, 105 unità/mL lattato deidrogenasi e 0,5 mM di peptide substrato (sequenza: EAIYAAPFAKKK). Le reazioni (75 μL) vengono avviate aggiungendo una quantità sufficiente di chinasi per portare le reazioni a una concentrazione di chinasi di 30 nM e la diminuzione dell'assorbanza viene monitorata per 30 minuti a 30°C in uno spettrofotometro per micropiastre. Le costanti inibitorie sono ottenute mediante l'aggiunta di 3,75 μL di Tozasertib (VX-680) in DMSO al 100% o solo DMSO. I valori di Ki sono calcolati come segue: K i = IC50 / (1 + [S]/Kd), dove [S] = [ATP] = 2,2 mM, e Kd (dell'ATP all'Abl) = 70 μM. Questi valori sono calcolati assumendo un Kd (ATP) di 70 μM per il dominio chinasico Abl di tipo selvaggio e H396P.
|
|
| In vivo |
Tozasertib (VX-680) provoca una marcata diminuzione delle dimensioni del tumore in un modello di xenotrapianto di AML umana (HL-60). Nei topi nudi trattati con esso a 75 mg/kg, due volte al giorno per via intraperitoneale (b.i.d. i.p.) per 13 giorni, i volumi medi del tumore sono ridotti del 98%. La diminuzione della crescita tumorale è dose-dipendente e significativa a una dose di 12,5 mg/kg b.i.d. Questo composto è ben tollerato, con una piccola diminuzione del peso corporeo osservata solo alla dose più alta. Innesca anche la regressione tumorale in modelli di xenotrapianto pancreatici e del colon. Tozasertib mostra anche una potente attività antitumorale se infuso per via endovenosa in ratti nudi portatori di tumori HCT116 consolidati. Una dose più alta (2 mg/kg/h) migliora l'efficacia con una diminuzione del 56% del volume tumorale medio.
|
Riferimenti |
|
Applicazioni
| Metodi | Biomarcatori | Immagini | PMID |
|---|---|---|---|
| Western blot | DLK / p-MKK7 / MKK7 / p-JNK / JNK p-AURKA / AURKA / Survivin YAP p-AKT / p-GSK3β / Cleaved caspase-3 / Cleaved PARP |
|
23431148 |
| Immunofluorescence | α-tubulin / Aurora-A |
|
21600017 |
| Growth inhibition assay | Cell viability |
|
21600017 |
Informazioni sullo studio clinico
(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)
| Numero NCT | Reclutamento | Condizioni | Sponsor/Collaboratori | Data di inizio | Fasi |
|---|---|---|---|---|---|
| NCT00290550 | Terminated | Carcinoma Non-Small-Cell Lung |
Merck Sharp & Dohme LLC |
June 2006 | Phase 2 |
| NCT00111683 | Completed | Chronic Myelogenous Leukemia in Blast Crisis|Lymphocytic Leukemia B Cell Acute|Myelodysplastic Syndromes|Myelogenous Leukemia Chronic |
Merck Sharp & Dohme LLC |
June 2005 | Phase 1 |
Supporto tecnico
Istruzioni per la manipolazione
Tel: +1-832-582-8158 Ext:3
Per qualsiasi altra domanda, si prega di lasciare un messaggio.
I prodotti sono solo per uso di ricerca. Non per uso umano. Non vendiamo a pazienti.
©Copyright 2013 Selleck Chemicals. Tutti i diritti riservati.