solo per uso di ricerca
PD173074 FGFR1 inhibitor
N. Cat.: S1264
Struttura chimica
Peso molecolare: 523.67
Vai a
Controllo Qualità (Quality Control)
Lotto:
Purezza:
99.95%
99.95
| Target correlati | EGFR VEGFR JAK PDGFR Src HIF FLT3 FLT HER2 Bcr-Abl |
|---|---|
| Altro FGFR Inibitori | AZD4547 (Fexagratinib) BLU9931 Futibatinib (TAS-120) LY2874455 PD-166866 H3B-6527 Zoligratinib (Debio-1347) Fisogatinib (BLU-554) SSR128129E Ferulic Acid |
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 |
|---|---|---|---|---|---|---|
| NCI-H1581 | Growth Inhibition Assay | IC50=0.01225 μM | SANGER | |||
| KG-1 | Growth Inhibition Assay | IC50=0.05129 μM | SANGER | |||
| MFM-223 | Growth Inhibition Assay | IC50=0.21576 μM | SANGER | |||
| EoL-1-cell | Growth Inhibition Assay | IC50=0.32984 μM | SANGER | |||
| ECC10 | Growth Inhibition Assay | IC50=0.33898 μM | SANGER | |||
| H-EMC-SS | Growth Inhibition Assay | IC50=0.34715 μM | SANGER | |||
| AN3-CA | Growth Inhibition Assay | IC50=0.40133 μM | SANGER | |||
| HuO-3N1 | Growth Inhibition Assay | IC50=0.54653 μM | SANGER | |||
| RT-112 | Growth Inhibition Assay | IC50=0.54701 μM | SANGER | |||
| NEC8 | Growth Inhibition Assay | IC50=0.56289 μM | SANGER | |||
| D-263MG | Growth Inhibition Assay | IC50=0.71159 μM | SANGER | |||
| SW962 | Growth Inhibition Assay | IC50=0.78988 μM | SANGER | |||
| BV-173 | Growth Inhibition Assay | IC50=0.84623 μM | SANGER | |||
| MFE-280 | Growth Inhibition Assay | IC50=0.85872 μM | SANGER | |||
| HuH-7 | Growth Inhibition Assay | IC50=1.24464 μM | SANGER | |||
| RS4-11 | Growth Inhibition Assay | IC50=1.33886 μM | SANGER | |||
| DMS-114 | Growth Inhibition Assay | IC50=1.36737 μM | SANGER | |||
| MSTO-211H | Growth Inhibition Assay | IC50=1.47378 μM | SANGER | |||
| DU-145 | Growth Inhibition Assay | IC50=1.58217 μM | SANGER | |||
| A172 | Growth Inhibition Assay | IC50=1.70355 μM | SANGER | |||
| SBC-1 | Growth Inhibition Assay | IC50=2.094 μM | SANGER | |||
| H9 | Growth Inhibition Assay | IC50=2.14306 μM | SANGER | |||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=2.18394 μM | SANGER | |||
| NCI-H720 | Growth Inhibition Assay | IC50=2.21283 μM | SANGER | |||
| HCC2218 | Growth Inhibition Assay | IC50=2.37939 μM | SANGER | |||
| G-401 | Growth Inhibition Assay | IC50=2.47189 μM | SANGER | |||
| MPP-89 | Growth Inhibition Assay | IC50=2.48364 μM | SANGER | |||
| 697 | Growth Inhibition Assay | IC50=2.65331 μM | SANGER | |||
| KARPAS-45 | Growth Inhibition Assay | IC50=2.70747 μM | SANGER | |||
| MG-63 | Growth Inhibition Assay | IC50=2.94262 μM | SANGER | |||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=3.03472 μM | SANGER | |||
| G-402 | Growth Inhibition Assay | IC50=3.12727 μM | SANGER | |||
| NKM-1 | Growth Inhibition Assay | IC50=3.13564 μM | SANGER | |||
| RH-18 | Growth Inhibition Assay | IC50=3.19598 μM | SANGER | |||
| NCI-H1092 | Growth Inhibition Assay | IC50=3.1969 μM | SANGER | |||
| RPMI-8226 | Growth Inhibition Assay | IC50=3.23447 μM | SANGER | |||
| GAMG | Growth Inhibition Assay | IC50=3.46576 μM | SANGER | |||
| HH | Growth Inhibition Assay | IC50=3.47676 μM | SANGER | |||
| RO82-W-1 | Growth Inhibition Assay | IC50=3.49855 μM | SANGER | |||
| CCRF-CEM | Growth Inhibition Assay | IC50=3.50488 μM | SANGER | |||
| NBsusSR | Growth Inhibition Assay | IC50=3.63969 μM | SANGER | |||
| CHL-1 | Growth Inhibition Assay | IC50=3.65799 μM | SANGER | |||
| LK-2 | Growth Inhibition Assay | IC50=3.67133 μM | SANGER | |||
| Hs-578-T | Growth Inhibition Assay | IC50=3.67873 μM | SANGER | |||
| CTB-1 | Growth Inhibition Assay | IC50=3.80051 μM | SANGER | |||
| ES5 | Growth Inhibition Assay | IC50=3.83637 μM | SANGER | |||
| A204 | Growth Inhibition Assay | IC50=3.92075 μM | SANGER | |||
| SW780 | Growth Inhibition Assay | IC50=3.92245 μM | SANGER | |||
| EW-3 | Growth Inhibition Assay | IC50=3.98923 μM | SANGER | |||
| A704 | Growth Inhibition Assay | IC50=4.28723 μM | SANGER | |||
| LU-139 | Growth Inhibition Assay | IC50=4.31534 μM | SANGER | |||
| CAL-72 | Growth Inhibition Assay | IC50=4.41746 μM | SANGER | |||
| D-336MG | Growth Inhibition Assay | IC50=4.46817 μM | SANGER | |||
| LAMA-84 | Growth Inhibition Assay | IC50=4.5331 μM | SANGER | |||
| GI-ME-N | Growth Inhibition Assay | IC50=4.5481 μM | SANGER | |||
| KM-H2 | Growth Inhibition Assay | IC50=4.55222 μM | SANGER | |||
| NCI-H209 | Growth Inhibition Assay | IC50=4.58283 μM | SANGER | |||
| IGROV-1 | Growth Inhibition Assay | IC50=4.87168 μM | SANGER | |||
| L-363 | Growth Inhibition Assay | IC50=4.96665 μM | SANGER | |||
| SK-MEL-3 | Growth Inhibition Assay | IC50=5.2406 μM | SANGER | |||
| HuO9 | Growth Inhibition Assay | IC50=5.38843 μM | SANGER | |||
| NOS-1 | Growth Inhibition Assay | IC50=5.72927 μM | SANGER | |||
| NCI-H1770 | Growth Inhibition Assay | IC50=5.95032 μM | SANGER | |||
| SF126 | Growth Inhibition Assay | IC50=6.21406 μM | SANGER | |||
| ML-2 | Growth Inhibition Assay | IC50=6.24977 μM | SANGER | |||
| CHP-134 | Growth Inhibition Assay | IC50=6.25182 μM | SANGER | |||
| NCI-H1355 | Growth Inhibition Assay | IC50=6.41733 μM | SANGER | |||
| TE-12 | Growth Inhibition Assay | IC50=6.72671 μM | SANGER | |||
| A4-Fuk | Growth Inhibition Assay | IC50=6.73142 μM | SANGER | |||
| MV-4-11 | Growth Inhibition Assay | IC50=6.76626 μM | SANGER | |||
| SK-UT-1 | Growth Inhibition Assay | IC50=6.91784 μM | SANGER | |||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=7.07764 μM | SANGER | |||
| ME-180 | Growth Inhibition Assay | IC50=7.10404 μM | SANGER | |||
| SK-MEL-28 | Growth Inhibition Assay | IC50=7.37819 μM | SANGER | |||
| HAL-01 | Growth Inhibition Assay | IC50=7.48341 μM | SANGER | |||
| ES8 | Growth Inhibition Assay | IC50=7.69626 μM | SANGER | |||
| DB | Growth Inhibition Assay | IC50=8.11504 μM | SANGER | |||
| SK-NEP-1 | Growth Inhibition Assay | IC50=8.48149 μM | SANGER | |||
| COR-L88 | Growth Inhibition Assay | IC50=8.50981 μM | SANGER | |||
| LB1047-RCC | Growth Inhibition Assay | IC50=8.52212 μM | SANGER | |||
| NCI-H520 | Growth Inhibition Assay | IC50=8.62157 μM | SANGER | |||
| SW954 | Growth Inhibition Assay | IC50=8.69786 μM | SANGER | |||
| TE-6 | Growth Inhibition Assay | IC50=8.75143 μM | SANGER | |||
| D-283MED | Growth Inhibition Assay | IC50=9.06534 μM | SANGER | |||
| DBTRG-05MG | Growth Inhibition Assay | IC50=9.09607 μM | SANGER | |||
| NCI-H446 | Growth Inhibition Assay | IC50=9.29526 μM | SANGER | |||
| HOS | Growth Inhibition Assay | IC50=9.35134 μM | SANGER | |||
| ES4 | Growth Inhibition Assay | IC50=9.50595 μM | SANGER | |||
| EW-13 | Growth Inhibition Assay | IC50=9.89055 μM | SANGER | |||
| IST-MES1 | Growth Inhibition Assay | IC50=9.94534 μM | SANGER | |||
| CAS-1 | Growth Inhibition Assay | IC50=9.97659 μM | SANGER | |||
| EM-2 | Growth Inhibition Assay | IC50=10.1393 μM | SANGER | |||
| SW948 | Growth Inhibition Assay | IC50=10.1882 μM | SANGER | |||
| OAW-42 | Growth Inhibition Assay | IC50=10.5267 μM | SANGER | |||
| BE-13 | Growth Inhibition Assay | IC50=10.6576 μM | SANGER | |||
| KU812 | Growth Inhibition Assay | IC50=10.7391 μM | SANGER | |||
| SK-MEL-30 | Growth Inhibition Assay | IC50=10.8901 μM | SANGER | |||
| A2780 | Growth Inhibition Assay | IC50=11.0308 μM | SANGER | |||
| TGBC24TKB | Growth Inhibition Assay | IC50=11.0737 μM | SANGER | |||
| GOTO | Growth Inhibition Assay | IC50=11.2084 μM | SANGER | |||
| NCI-H526 | Growth Inhibition Assay | IC50=11.3837 μM | SANGER | |||
| BHT-101 | Growth Inhibition Assay | IC50=11.4456 μM | SANGER | |||
| NCI-H1155 | Growth Inhibition Assay | IC50=11.4947 μM | SANGER | |||
| MCF7 | Growth Inhibition Assay | IC50=11.6167 μM | SANGER | |||
| MKN45 | Growth Inhibition Assay | IC50=11.7993 μM | SANGER | |||
| MOLT-16 | Growth Inhibition Assay | IC50=11.9692 μM | SANGER | |||
| YH-13 | Growth Inhibition Assay | IC50=12.0346 μM | SANGER | |||
| P12-ICHIKAWA | Growth Inhibition Assay | IC50=12.3845 μM | SANGER | |||
| GR-ST | Growth Inhibition Assay | IC50=12.5295 μM | SANGER | |||
| CAKI-1 | Growth Inhibition Assay | IC50=12.791 μM | SANGER | |||
| LXF-289 | Growth Inhibition Assay | IC50=13.0835 μM | SANGER | |||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=13.2704 μM | SANGER | |||
| EW-16 | Growth Inhibition Assay | IC50=13.3187 μM | SANGER | |||
| NCI-H82 | Growth Inhibition Assay | IC50=13.4195 μM | SANGER | |||
| MMAC-SF | Growth Inhibition Assay | IC50=13.4547 μM | SANGER | |||
| COLO-684 | Growth Inhibition Assay | IC50=13.5318 μM | SANGER | |||
| QIMR-WIL | Growth Inhibition Assay | IC50=13.8109 μM | SANGER | |||
| NB69 | Growth Inhibition Assay | IC50=13.9868 μM | SANGER | |||
| NCI-H2291 | Growth Inhibition Assay | IC50=14.4453 μM | SANGER | |||
| MKN7 | Growth Inhibition Assay | IC50=14.6676 μM | SANGER | |||
| HDLM-2 | Growth Inhibition Assay | IC50=15.1286 μM | SANGER | |||
| A253 | Growth Inhibition Assay | IC50=15.3869 μM | SANGER | |||
| SK-LU-1 | Growth Inhibition Assay | IC50=15.9094 μM | SANGER | |||
| MEG-01 | Growth Inhibition Assay | IC50=15.9107 μM | SANGER | |||
| SK-N-DZ | Growth Inhibition Assay | IC50=15.9376 μM | SANGER | |||
| H4 | Growth Inhibition Assay | IC50=16.088 μM | SANGER | |||
| LU-65 | Growth Inhibition Assay | IC50=16.3384 μM | SANGER | |||
| NCI-H1048 | Growth Inhibition Assay | IC50=16.5165 μM | SANGER | |||
| LCLC-97TM1 | Growth Inhibition Assay | IC50=16.5889 μM | SANGER | |||
| CAL-120 | Growth Inhibition Assay | IC50=16.9879 μM | SANGER | |||
| LU-134-A | Growth Inhibition Assay | IC50=17.3391 μM | SANGER | |||
| SK-MEL-1 | Growth Inhibition Assay | IC50=17.7127 μM | SANGER | |||
| NCI-H69 | Growth Inhibition Assay | IC50=17.9307 μM | SANGER | |||
| MC116 | Growth Inhibition Assay | IC50=17.975 μM | SANGER | |||
| UMC-11 | Growth Inhibition Assay | IC50=18.1788 μM | SANGER | |||
| HCC1395 | Growth Inhibition Assay | IC50=18.4301 μM | SANGER | |||
| no-10 | Growth Inhibition Assay | IC50=18.6388 μM | SANGER | |||
| NY | Growth Inhibition Assay | IC50=19.0809 μM | SANGER | |||
| OS-RC-2 | Growth Inhibition Assay | IC50=19.1252 μM | SANGER | |||
| D-423MG | Growth Inhibition Assay | IC50=19.3952 μM | SANGER | |||
| LC-2-ad | Growth Inhibition Assay | IC50=19.7612 μM | SANGER | |||
| DU-4475 | Growth Inhibition Assay | IC50=19.8852 μM | SANGER | |||
| YKG-1 | Growth Inhibition Assay | IC50=19.962 μM | SANGER | |||
| HCC1569 | Growth Inhibition Assay | IC50=20.2624 μM | SANGER | |||
| TYK-nu | Growth Inhibition Assay | IC50=20.2847 μM | SANGER | |||
| DEL | Growth Inhibition Assay | IC50=20.9808 μM | SANGER | |||
| MHH-ES-1 | Growth Inhibition Assay | IC50=21.3597 μM | SANGER | |||
| KARPAS-299 | Growth Inhibition Assay | IC50=21.529 μM | SANGER | |||
| CTV-1 | Growth Inhibition Assay | IC50=21.6172 μM | SANGER | |||
| NCI-H2452 | Growth Inhibition Assay | IC50=22.6677 μM | SANGER | |||
| D-566MG | Growth Inhibition Assay | IC50=22.7601 μM | SANGER | |||
| EFO-27 | Growth Inhibition Assay | IC50=23.0651 μM | SANGER | |||
| NCI-H596 | Growth Inhibition Assay | IC50=23.8527 μM | SANGER | |||
| KS-1 | Growth Inhibition Assay | IC50=24.2759 μM | SANGER | |||
| 8305C | Growth Inhibition Assay | IC50=24.4045 μM | SANGER | |||
| A427 | Growth Inhibition Assay | IC50=25.0323 μM | SANGER | |||
| COLO-800 | Growth Inhibition Assay | IC50=25.1061 μM | SANGER | |||
| SJRH30 | Growth Inhibition Assay | IC50=25.3908 μM | SANGER | |||
| MEL-HO | Growth Inhibition Assay | IC50=25.4319 μM | SANGER | |||
| FTC-133 | Growth Inhibition Assay | IC50=25.8186 μM | SANGER | |||
| SF295 | Growth Inhibition Assay | IC50=26.296 μM | SANGER | |||
| SW1710 | Growth Inhibition Assay | IC50=26.4123 μM | SANGER | |||
| EFM-19 | Growth Inhibition Assay | IC50=26.8145 μM | SANGER | |||
| NB10 | Growth Inhibition Assay | IC50=28.2297 μM | SANGER | |||
| TK10 | Growth Inhibition Assay | IC50=28.2399 μM | SANGER | |||
| D-502MG | Growth Inhibition Assay | IC50=28.4 μM | SANGER | |||
| EW-18 | Growth Inhibition Assay | IC50=28.4386 μM | SANGER | |||
| VMRC-RCZ | Growth Inhibition Assay | IC50=28.941 μM | SANGER | |||
| Ca9-22 | Growth Inhibition Assay | IC50=29.4557 μM | SANGER | |||
| KYSE-70 | Growth Inhibition Assay | IC50=29.5786 μM | SANGER | |||
| A101D | Growth Inhibition Assay | IC50=29.6472 μM | SANGER | |||
| WM-115 | Growth Inhibition Assay | IC50=29.7607 μM | SANGER | |||
| HCC2157 | Growth Inhibition Assay | IC50=29.8807 μM | SANGER | |||
| TE-9 | Growth Inhibition Assay | IC50=29.8865 μM | SANGER | |||
| K-562 | Growth Inhibition Assay | IC50=30.0933 μM | SANGER | |||
| SN12C | Growth Inhibition Assay | IC50=30.1426 μM | SANGER | |||
| ESS-1 | Growth Inhibition Assay | IC50=30.4759 μM | SANGER | |||
| K5 | Growth Inhibition Assay | IC50=30.764 μM | SANGER | |||
| J82 | Growth Inhibition Assay | IC50=31.0897 μM | SANGER | |||
| HOP-92 | Growth Inhibition Assay | IC50=31.1111 μM | SANGER | |||
| NCI-H2228 | Growth Inhibition Assay | IC50=31.3296 μM | SANGER | |||
| OCI-AML2 | Growth Inhibition Assay | IC50=31.361 μM | SANGER | |||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=31.8137 μM | SANGER | |||
| A3-KAW | Growth Inhibition Assay | IC50=31.9243 μM | SANGER | |||
| LCLC-103H | Growth Inhibition Assay | IC50=32.0171 μM | SANGER | |||
| KY821 | Growth Inhibition Assay | IC50=32.6884 μM | SANGER | |||
| JVM-2 | Growth Inhibition Assay | IC50=32.9079 μM | SANGER | |||
| Mo-T | Growth Inhibition Assay | IC50=33.1005 μM | SANGER | |||
| IA-LM | Growth Inhibition Assay | IC50=33.275 μM | SANGER | |||
| C8166 | Growth Inhibition Assay | IC50=33.3192 μM | SANGER | |||
| TCCSUP | Growth Inhibition Assay | IC50=33.4307 μM | SANGER | |||
| JEG-3 | Growth Inhibition Assay | IC50=33.4768 μM | SANGER | |||
| MS-1 | Growth Inhibition Assay | IC50=33.5551 μM | SANGER | |||
| NCI-H1304 | Growth Inhibition Assay | IC50=33.5725 μM | SANGER | |||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=34.0335 μM | SANGER | |||
| MDA-MB-453 | Growth Inhibition Assay | IC50=34.6395 μM | SANGER | |||
| KYSE-520 | Growth Inhibition Assay | IC50=34.7181 μM | SANGER | |||
| SW900 | Growth Inhibition Assay | IC50=34.8115 μM | SANGER | |||
| HCC2998 | Growth Inhibition Assay | IC50=35.1529 μM | SANGER | |||
| A2058 | Growth Inhibition Assay | IC50=35.6061 μM | SANGER | |||
| OVCAR-3 | Growth Inhibition Assay | IC50=36.2045 μM | SANGER | |||
| MOLT-4 | Growth Inhibition Assay | IC50=36.2294 μM | SANGER | |||
| CAPAN-1 | Growth Inhibition Assay | IC50=36.4699 μM | SANGER | |||
| SCC-9 | Growth Inhibition Assay | IC50=37.4027 μM | SANGER | |||
| SF268 | Growth Inhibition Assay | IC50=38.3433 μM | SANGER | |||
| HGC-27 | Growth Inhibition Assay | IC50=38.3711 μM | SANGER | |||
| DOHH-2 | Growth Inhibition Assay | IC50=38.7158 μM | SANGER | |||
| KE-37 | Growth Inhibition Assay | IC50=38.9828 μM | SANGER | |||
| MOLT-13 | Growth Inhibition Assay | IC50=39.2502 μM | SANGER | |||
| ES1 | Growth Inhibition Assay | IC50=39.385 μM | SANGER | |||
| SK-OV-3 | Growth Inhibition Assay | IC50=39.9643 μM | SANGER | |||
| SNU-449 | Growth Inhibition Assay | IC50=40.0764 μM | SANGER | |||
| KYSE-510 | Growth Inhibition Assay | IC50=40.1295 μM | SANGER | |||
| HL-60 | Growth Inhibition Assay | IC50=40.9783 μM | SANGER | |||
| DJM-1 | Growth Inhibition Assay | IC50=40.9799 μM | SANGER | |||
| TGBC11TKB | Growth Inhibition Assay | IC50=41.0926 μM | SANGER | |||
| U-2-OS | Growth Inhibition Assay | IC50=42.2641 μM | SANGER | |||
| NCI-H2030 | Growth Inhibition Assay | IC50=42.4368 μM | SANGER | |||
| LU-135 | Growth Inhibition Assay | IC50=42.5447 μM | SANGER | |||
| ZR-75-30 | Growth Inhibition Assay | IC50=43.0493 μM | SANGER | |||
| GT3TKB | Growth Inhibition Assay | IC50=43.2679 μM | SANGER | |||
| RPMI-2650 | Growth Inhibition Assay | IC50=43.7816 μM | SANGER | |||
| SAS | Growth Inhibition Assay | IC50=43.9534 μM | SANGER | |||
| MDA-MB-231 | Growth Inhibition Assay | IC50=43.9609 μM | SANGER | |||
| JVM-3 | Growth Inhibition Assay | IC50=44.0533 μM | SANGER | |||
| COLO-320-HSR | Growth Inhibition Assay | IC50=44.5633 μM | SANGER | |||
| SNB75 | Growth Inhibition Assay | IC50=44.6105 μM | SANGER | |||
| NCI-H441 | Growth Inhibition Assay | IC50=44.9328 μM | SANGER | |||
| HCT-116 | Growth Inhibition Assay | IC50=44.9868 μM | SANGER | |||
| NCI-H226 | Growth Inhibition Assay | IC50=45.6368 μM | SANGER | |||
| CAL-33 | Growth Inhibition Assay | IC50=45.9217 μM | SANGER | |||
| NCI-H1437 | Growth Inhibition Assay | IC50=46.321 μM | SANGER | |||
| HCC1187 | Growth Inhibition Assay | IC50=46.4255 μM | SANGER | |||
| NUGC-3 | Growth Inhibition Assay | IC50=46.5709 μM | SANGER | |||
| T98G | Growth Inhibition Assay | IC50=47.547 μM | SANGER | |||
| OVCAR-8 | Growth Inhibition Assay | IC50=47.683 μM | SANGER | |||
| LB2241-RCC | Growth Inhibition Assay | IC50=47.727 μM | SANGER | |||
| NCI-H358 | Growth Inhibition Assay | IC50=48.1152 μM | SANGER | |||
| PANC-08-13 | Growth Inhibition Assay | IC50=48.1853 μM | SANGER | |||
| KP-N-YN | Growth Inhibition Assay | IC50=48.2102 μM | SANGER | |||
| NCI-H1755 | Growth Inhibition Assay | IC50=48.2726 μM | SANGER | |||
| NCI-N87 | Growth Inhibition Assay | IC50=48.2991 μM | SANGER | |||
| SUM52 | Antiproliferative assay | 5 days | Antiproliferative activity against human FGFR2-amplified SUM52 cells after 5 days by SRB assay, IC50 = 0.0123 μM. | 28521156 | ||
| RT112 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human RT112 cells after 72 hrs by MTT assay, GI50 = 0.015 μM. | 27599742 | ||
| insect cells | Function assay | 10 mins | Inhibition of recombinant full length human FGFR1 expressed in baculovirus infected insect cells in presence of [gamma-32P]ATP after 10 mins by scintillation counting based radioactive filter binding assay, IC50 = 0.0215 μM. | 27914362 | ||
| SW780 | Antiproliferative assay | 5 days | Antiproliferative activity against human FGFR3-amplified SW780 cells after 5 days by SRB assay, IC50 = 0.0843 μM. | 28521156 | ||
| NIH/ 3T3 | Function assay | 5 mins | Inhibition of VEGFR2 (unknown origin) overexpressed in mouse NIH/ 3T3 cells incubated for 5 mins followed by stimulation with VEGF for 5 mins by immunoblotting analysis, IC50 = 0.1 μM. | 27326339 | ||
| NCI-H520 | Antiproliferative assay | 7 days | Antiproliferative activity against human FGFR1-amplified NCI-H520 cells after 7 days by SRB assay, IC50 = 0.281 μM. | 28521156 | ||
| HUVEC | Function assay | 10 nM | 14 hrs | Inhibition of FGFR-mediated angiogenesis in human HUVEC cells assessed as decrease in capillary tube sprouting at 10 nM after 14 hrs | 16474387 | |
| HUVEC | Function assay | 100 nM | 14 hrs | Inhibition of FGFR-mediated angiogenesis in human HUVEC cells assessed as decrease in capillary tube sprouting at 100 nM after 14 hrs | 16474387 | |
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 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 | |||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 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 | |||
| 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 | |||
| fibroblast cells | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 29435139 | |||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | |||
| Clicca per visualizzare più dati sperimentali sulle linee cellulari | ||||||
Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)
| Peso molecolare | 523.67 | Formula | C28H41N7O3 |
Conservazione (Dalla data di ricezione) | |
|---|---|---|---|---|---|
| N. CAS | 219580-11-7 | Scarica SDF | Conservazione delle soluzioni stock |
|
|
| Sinonimi | N/A | Smiles | CCN(CC)CCCCNC1=NC2=NC(=C(C=C2C=N1)C3=CC(=CC(=C3)OC)OC)NC(=O)NC(C)(C)C | ||
Solubilità (Solubility)
|
In vitro |
DMSO
: 105 mg/mL
(200.5 mM)
Ethanol : 105 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 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)
| Targets/IC50/Ki |
FGFR1
(Cell-free assay) ~25 nM
VEGFR2
(Cell-free assay) 100 nM-200 nM
|
|---|---|
| In vitro |
PD173074 è un inibitore di FGFR1 competitivo con ATP con un Ki di ~40 nM. Questo composto è anche un efficace inibitore di VEGFR2. Rispetto a FGFR1, inibisce debolmente le attività di Src, InsR, EGFR, PDGFR, MEK e PKC con valori di IC50 1000 volte o maggiori. Questo inibitore inibisce l'autofosforilazione di FGFR1 e VEGFR2 in modo dose-dipendente con IC50 di 1-5 nM e 100-200 nM, rispettivamente. Inibisce la promozione della sopravvivenza dei neuroni granulari da parte di FGF-2 in modo dose-dipendente con IC50 di 12 nM, mostrando una potenza 1.000 volte maggiore rispetto a quella di SU 5402. Questa sostanza chimica inibisce specificamente gli effetti mediati da FGF-2 sulla proliferazione, differenziazione e attivazione di MAPK nelle cellule della linea oligodendrocitica (OL). È attivo contro il recettore WT e le mutazioni di FGFR3 nelle linee cellulari di mieloma multiplo (MM). Questo composto inibisce anche potentemente l'autofosforilazione di FGFR3 in modo dose-dipendente con IC50 di ~5 nM. Il suo trattamento riduce potentemente la vitalità delle cellule KMS11 e KMS18 che esprimono FGFR3 con IC50 <20 nM. L'inibizione della crescita delle cellule MM stimolate da aFGF da parte di questo agente è altamente correlata all'espressione di FGFR3. Il suo trattamento abolisce completamente la trasformazione delle cellule NIH 3T3 mediata da Y373C FGFR3 ma non da Ras V12, dimostrando che mira specificamente alla trasformazione cellulare mediata da FGFR3 e manca di effetti citotossici non specifici. Questa sostanza chimica induce anche la maturazione funzionale delle cellule KMS11 e KMS18.
|
| Saggio chinasico |
Saggi di inibizione chinasica in vitro
|
|
I saggi che utilizzano la chinasi FGFR-1 a lunghezza intera vengono eseguiti in un volume totale di 100 μL contenente 25 mM di tampone HEPES (pH 7,4), 150 mM di NaCl, 10 mM di MnCl2, 0,2 mM di ortovanadato di sodio, 750 μg/mL di una concentrazione di un copolimero casuale di acido glutammico e tirosina (4:1), varie concentrazioni di PD173074 e 60-75 ng di enzima. La reazione viene avviata con l'aggiunta di [γ-32P]ATP (5 μM ATP contenente 0,4 μCi di [γ-32P]ATP per incubazione), e i campioni vengono incubati a 25°C per 10 minuti. La reazione viene terminata con l'aggiunta del 30% di acido tricloroacetico e la precipitazione del materiale su tappetini filtranti in fibra di vetro. I filtri vengono lavati tre volte con il 15% di acido tricloroacetico, e l'incorporazione di [32P] nel substrato polimerico di glutammato tirosina viene determinata contando la radioattività trattenuta sui filtri in un lettore di betapiastre Wallac 1250. L'attività non specifica è definita come la radioattività trattenuta sui filtri dopo l'incubazione dei campioni senza enzima. L'attività specifica è determinata come l'attività totale (enzima più tampone) meno l'attività non specifica. La concentrazione di questo composto che inibisce l'attività enzimatica di FGFR-1 del 50% (IC50) viene determinata graficamente.
|
|
| In vivo |
L'amministrazione di PD173074 a 1 mg/kg/giorno o 2 mg/kg/giorno nei topi può bloccare efficacemente l'Angiogenesis indotta da FGF o VEGF in modo dose-dipendente senza tossicità apparente. Questo composto inibisce la crescita in vivo di cellule NIH 3T3 transfettate con FGFR3 mutante in topi nudi. L'inibizione di FGFR3 da parte di questa sostanza chimica ritarda la crescita tumorale e aumenta la sopravvivenza dei topi in un modello di mieloma di xenotrapianto KMS11. Nel xenotrapianto H-510, la somministrazione orale di questo composto blocca la crescita tumorale in modo simile a quanto osservato con la somministrazione di cisplatino in monoterapia, aumentando la sopravvivenza mediana rispetto agli animali di controllo trattati con simulazione. Nei xenotrapianti H-69, questa sostanza chimica induce risposte complete che durano >6 mesi nel 50% dei topi. Questi effetti sono correlati a un aumento dell'apoptosi nei tumori escissi, ma non sono una conseguenza della disruzione della vascolarizzazione tumorale.
|
Riferimenti |
|
Applicazioni (Applications)
| Metodi | Biomarcatori | Immagini | PMID |
|---|---|---|---|
| Western blot | pFGFR2 / FGFR2 p-S6RP / p-PRAS40 / p-p105 NFKB / P105 NFKB / P50 NFKB / p-AMPK / p-CRK II / p-PDK1 |
|
24968263 |
| Growth inhibition assay | Cell viability |
|
24968263 |
Domande Frequenti (Frequently Asked Questions)
Domanda 1:
What is the half-life of this compound (S1264) in vivo?
Risposta:
According to literature research, it is given twice daily because this compound has a short half-life in vivo, please refer to the following link for detailed pharmacokinetic information (Supplementary Figure 8B): http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3990281/#!po=50.0000.
I prodotti sono solo per uso di ricerca. Non per uso umano. Non vendiamo a pazienti.
©Copyright 2013 Selleck Chemicals. Tutti i diritti riservati.