solo para uso en investigación
PD173074 inhibidor de FGFR1
Cat. No.S1264
Estructura química
Peso molecular: 523.67
Saltar a
Control de calidad (Quality Control)
Lote:
Pureza:
99.95%
99.95
| Dianas relacionadas | EGFR VEGFR JAK PDGFR Src HIF FLT FLT3 HER2 Bcr-Abl |
|---|---|
| Otros FGFR Inhibidores | AZD4547 (Fexagratinib) BLU9931 Futibatinib (TAS-120) LY2874455 PD-166866 H3B-6527 Zoligratinib (Debio-1347) Fisogatinib (BLU-554) SSR128129E Ferulic Acid |
Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)
| Líneas celulares | Tipo de ensayo | Concentración | Tiempo de incubación | Formulación | Descripción de la actividad | 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 | |||
| Haga clic para ver más datos experimentales de líneas celulares | ||||||
Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)
| Peso molecular | 523.67 | Fórmula | C28H41N7O3 |
Almacenamiento (Desde la fecha de recepción) | |
|---|---|---|---|---|---|
| Nº CAS | 219580-11-7 | Descargar SDF | Almacenamiento de soluciones madre |
|
|
| Sinónimos | N/A | Smiles | CCN(CC)CCCCNC1=NC2=NC(=C(C=C2C=N1)C3=CC(=CC(=C3)OC)OC)NC(=O)NC(C)(C)C | ||
Solubilidad (Solubility)
|
In vitro |
DMSO
: 105 mg/mL
(200.5 mM)
Ethanol : 105 mg/mL Water : Insoluble |
Calculadora de Molaridad
Calculadora de Dilución
Calculadora de Peso Molecular
|
In vivo |
|||||
Calculadora de formulación in vivo (Solución clara)
Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)
mg/kg
g
μL
Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Resultados del cálculo:
Concentración de trabajo: mg/ml;
Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )
Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH2O, mezclar y clarificar.
Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.
Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.
Mecanismo de acción (Mechanism of Action)
| Targets/IC50/Ki |
FGFR1
(Cell-free assay) ~25 nM
VEGFR2
(Cell-free assay) 100 nM-200 nM
|
|---|---|
| In vitro |
PD173074 es un inhibidor de FGFR1 competitivo con ATP con un Ki de ~40 nM. Este compuesto también es un inhibidor eficaz de VEGFR2. Comparado con FGFR1, inhibe débilmente las actividades de Src, InsR, EGFR, PDGFR, MEK y PKC con valores de IC50 1000 veces o mayores. Este inhibidor inhibe la autofosforilación de FGFR1 y VEGFR2 de manera dosis-dependiente con una IC50 de 1-5 nM y 100-200 nM, respectivamente. Inhibe la promoción de la supervivencia de neuronas granulares por FGF-2 de manera dosis-dependiente con una IC50 de 12 nM, exhibiendo una potencia 1.000 veces mayor que la de SU 5402. Este químico inhibe específicamente los efectos mediados por FGF-2 sobre la proliferación, diferenciación y activación de MAPK en células del linaje oligodendrocítico (OL). Es activo contra el receptor WT y las mutaciones de FGFR3 en líneas celulares de mieloma múltiple (MM). Este compuesto también inhibe potentemente la autofosforilación de FGFR3 de manera dosis-dependiente con una IC50 de ~5 nM. Su tratamiento reduce potentemente la viabilidad de las células KMS11 y KMS18 que expresan FGFR3 con una IC50 <20 nM. La inhibición del crecimiento de células MM estimuladas por aFGF por este agente está altamente correlacionada con la expresión de FGFR3. Su tratamiento anula completamente la transformación de NIH 3T3 mediada por Y373C FGFR3 pero no por Ras V12, demostrando que se dirige específicamente a la transformación celular mediada por FGFR3 y carece de efecto citotóxico no específico. Este químico también induce la maduración funcional de las células KMS11 y KMS18.
|
| Ensayo de quinasa |
Ensayos de inhibición de quinasa in vitro
|
|
Los ensayos que utilizan la quinasa FGFR-1 de longitud completa se realizan en un volumen total de 100 μL que contiene 25 mM de tampón HEPES (pH 7.4), 150 mM de NaCl, 10 mM de MnCl2, 0.2 mM de ortovanadato de sodio, 750 μg/mL de concentración de un copolímero aleatorio de ácido glutámico y tirosina (4:1), varias concentraciones de PD173074 y 60 a 75 ng de enzima. La reacción se inicia con la adición de [γ-32P]ATP (5 μM de ATP que contiene 0.4 μCi de [γ-32P]ATP por incubación), y las muestras se incuban a 25°C durante 10 minutos. La reacción se termina con la adición de 30% de ácido tricloroacético y la precipitación del material sobre tapetes filtrantes de fibra de vidrio. Los filtros se lavan tres veces con 15% de ácido tricloroacético, y la incorporación de [32P] en el sustrato de polímero de glutamato tirosina se determina contando la radioactividad retenida en los filtros en un lector de betaplatos Wallac 1250. La actividad no específica se define como la radioactividad retenida en los filtros después de la incubación de las muestras sin enzima. La actividad específica se determina como la actividad total (enzima más tampón) menos la actividad no específica. La concentración de este compuesto que inhibe la actividad enzimática de FGFR-1 en un 50% (IC50) se determina gráficamente.
|
|
| In vivo |
La administración de PD173074 a 1 mg/kg/día o 2 mg/kg/día en ratones puede bloquear eficazmente la Angiogenesis inducida por FGF o VEGF de manera dosis-dependiente sin toxicidad aparente. Este compuesto inhibe el crecimiento in vivo de células NIH 3T3 transfectadas con FGFR3 mutante en ratones desnudos. La inhibición de FGFR3 por este químico retrasa el crecimiento tumoral y aumenta la supervivencia de los ratones en un modelo de mieloma de xenoinjerto KMS11. En el xenoinjerto H-510, la administración oral de este compuesto bloquea el crecimiento tumoral de manera similar a la observada con la administración de cisplatino como agente único, aumentando la supervivencia media en comparación con los animales de control tratados simuladamente. En los xenoinjertos H-69, este químico induce respuestas completas que duran >6 meses en el 50% de los ratones. Estos efectos se correlacionan con un aumento de la apoptosis en los tumores extirpados, pero no son una consecuencia de la alteración de la vasculatura tumoral.
|
Referencias |
|
Aplicaciones (Applications)
| Métodos | Biomarcadores | Imágenes | 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 |
Preguntas frecuentes (Frequently Asked Questions)
Pregunta 1:
What is the half-life of this compound (S1264) in vivo?
Respuesta:
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.
Los productos son solo para uso de investigación. No para uso humano. No vendemos a pacientes.
©Copyright 2013 Selleck Chemicals. Todos los derechos reservados.