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PD173074 inhibiteur de FGFR1
Réf. CatalogueS1264
Structure chimique
Poids moléculaire: 523.67
Aller à
Contrôle Qualité
Lot :
Pureté :
99.95%
99.95
| Cibles apparentées | EGFR VEGFR JAK PDGFR Src HIF FLT FLT3 HER2 Bcr-Abl |
|---|---|
| Autre FGFR Inhibiteurs | AZD4547 (Fexagratinib) BLU9931 Futibatinib (TAS-120) LY2874455 PD-166866 Zoligratinib (Debio-1347) H3B-6527 Fisogatinib (BLU-554) SSR128129E Ferulic Acid |
Culture cellulaire, traitement et concentration de travail
| Lignées cellulaires | Type dessai | Concentration | Temps dincubation | Formulation | Description de lactivité | 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 | |||
| Cliquez pour voir plus de données expérimentales sur la lignée cellulaire | ||||||
Informations chimiques, stockage et stabilité
| Poids moléculaire | 523.67 | Formule | C28H41N7O3 |
Stockage (À compter de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 219580-11-7 | Télécharger le SDF | Stockage des solutions mères |
|
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| Synonymes | N/A | Smiles | CCN(CC)CCCCNC1=NC2=NC(=C(C=C2C=N1)C3=CC(=CC(=C3)OC)OC)NC(=O)NC(C)(C)C | ||
Solubilité
|
In vitro |
DMSO
: 105 mg/mL
(200.5 mM)
Ethanol : 105 mg/mL Water : Insoluble |
Calculateur de molarité
Calculateur de dilution
Calculateur de poids moléculaire
|
In vivo |
|||||
Calculateur de formulation in vivo (Solution claire)
Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)
mg/kg
g
μL
Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Résultats du calcul :
Concentration de travail : mg/ml;
Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH2O, mélanger et clarifier.
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.
Note : 1. Veuillez vous assurer que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue, lors de lajout précédent, est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.
Mécanisme daction
| Targets/IC50/Ki |
FGFR1
(Cell-free assay) ~25 nM
VEGFR2
(Cell-free assay) 100 nM-200 nM
|
|---|---|
| In vitro |
PD173074 est un inhibiteur de FGFR1 compétitif à l'ATP avec un Ki d'environ 40 nM. Ce composé est également un inhibiteur efficace de VEGFR2. Comparé à FGFR1, il inhibe faiblement les activités de Src, InsR, EGFR, PDGFR, MEK et PKC avec des valeurs IC50 1000 fois ou plus élevées. Cet inhibiteur inhibe l'autophosphorylation de FGFR1 et VEGFR2 de manière dose-dépendante avec une IC50 de 1-5 nM et 100-200 nM, respectivement. Il inhibe la promotion de la survie des neurones granulaires par le FGF-2 de manière dose-dépendante avec une IC50 de 12 nM, présentant une puissance 1 000 fois supérieure à celle du SU 5402. Ce produit chimique inhibe spécifiquement les effets médiés par le FGF-2 sur la prolifération, la différenciation et l'activation de la MAPK dans les cellules de la lignée oligodendrocytaire (OL). Il est actif contre le récepteur WT et les mutations de FGFR3 dans les lignées cellulaires de myélome multiple (MM). Ce composé inhibe également puissamment l'autophosphorylation de FGFR3 de manière dose-dépendante avec une IC50 d'environ 5 nM. Son traitement réduit puissamment la viabilité des cellules KMS11 et KMS18 exprimant FGFR3 avec une IC50 <20 nM. L'inhibition de la croissance des cellules MM stimulées par l'aFGF par cet agent est fortement corrélée à l'expression de FGFR3. Son traitement abolit complètement la transformation des NIH 3T3 médiée par Y373C FGFR3 mais pas par Ras V12, démontrant qu'il cible spécifiquement la transformation cellulaire médiée par FGFR3 et n'a pas d'effet cytotoxique non spécifique. Ce produit chimique induit également la maturation fonctionnelle des cellules KMS11 et KMS18.
|
| Essai kinase |
Tests d'inhibition de kinase in vitro
|
|
Des tests utilisant la kinase FGFR-1 pleine longueur sont réalisés dans un volume total de 100 μL contenant 25 mM de tampon HEPES (pH 7,4), 150 mM de NaCl, 10 mM de MnCl2, 0,2 mM d'orthovanadate de sodium, 750 μg/mL d'une concentration d'un copolymère aléatoire d'acide glutamique et de tyrosine (4:1), diverses concentrations de PD173074 et 60 à 75 ng d'enzyme. La réaction est initiée par l'addition de [γ-32P]ATP (5 μM d'ATP contenant 0,4 μCi de [γ-32P]ATP par incubation), et les échantillons sont incubés à 25°C pendant 10 minutes. La réaction est terminée par l'addition de 30% d'acide trichloroacétique et la précipitation du matériel sur des tapis filtrants en fibre de verre. Les filtres sont lavés trois fois avec 15% d'acide trichloroacétique, et l'incorporation de [32P] dans le substrat polymère de glutamate tyrosine est déterminée en comptant la radioactivité retenue sur les filtres dans un lecteur Wallac 1250 betaplate. L'activité non spécifique est définie comme la radioactivité retenue sur les filtres après incubation des échantillons sans enzyme. L'activité spécifique est déterminée comme l'activité totale (enzyme plus tampon) moins l'activité non spécifique. La concentration de ce composé qui inhibe l'activité enzymatique de FGFR-1 de 50% (IC50) est déterminée graphiquement.
|
|
| In vivo |
L'administration de PD173074 à 1 mg/kg/jour ou 2 mg/kg/jour chez la souris peut bloquer efficacement l'Angiogenesis induite par le FGF ou le VEGF de manière dose-dépendante sans toxicité apparente. Ce composé inhibe la croissance in vivo des cellules NIH 3T3 transfectées avec FGFR3 muté chez les souris nues. L'inhibition de FGFR3 par ce produit chimique retarde la croissance tumorale et augmente la survie des souris dans un modèle de myélome xénogreffe KMS11. Dans la xénogreffe H-510, l'administration orale de ce composé bloque la croissance tumorale de manière similaire à celle observée avec l'administration de cisplatine en monothérapie, augmentant la survie médiane par rapport aux animaux témoins traités par simulation. Dans les xénogreffes H-69, ce produit chimique induit des réponses complètes durant >6 mois chez 50% des souris. Ces effets sont corrélés à une augmentation de l'apoptose dans les tumeurs excisées, mais non à une conséquence d'une perturbation de la vascularisation tumorale.
|
Références |
|
Applications
| Méthodes | Biomarqueurs | Images | 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 |
Support technique
Tel: +1-832-582-8158 Ext:3
Si vous avez dautres questions, veuillez laisser un message.
Foire aux questions
Question 1:
What is the half-life of this compound (S1264) in vivo?
Réponse :
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.
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