nur für Forschungszwecke
PD173074 FGFR1-Inhibitor
Kat.-Nr.S1264
Chemische Struktur
Molekulargewicht: 523.67
Springe zu
Qualitätskontrolle
Charge:
Reinheit:
99.95%
99.95
| Verwandte Ziele | EGFR VEGFR JAK PDGFR Src HIF FLT FLT3 HER2 Bcr-Abl |
|---|---|
| Weitere FGFR Inhibitoren | AZD4547 (Fexagratinib) BLU9931 Futibatinib (TAS-120) LY2874455 PD-166866 Zoligratinib (Debio-1347) H3B-6527 Fisogatinib (BLU-554) SSR128129E Ferulic Acid |
Zellkultur, Behandlung & Arbeitskonzentration
| Zelllinien | Assay-Typ | Konzentration | Inkubationszeit | Formulierung | Aktivitätsbeschreibung | 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 | |||
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Chemische Informationen, Lagerung & Stabilität
| Molekulargewicht | 523.67 | Formel | C28H41N7O3 |
Lagerung (Ab dem Eingangsdatum) | |
|---|---|---|---|---|---|
| CAS-Nr. | 219580-11-7 | SDF herunterladen | Lagerung von Stammlösungen |
|
|
| Synonyme | N/A | Smiles | CCN(CC)CCCCNC1=NC2=NC(=C(C=C2C=N1)C3=CC(=CC(=C3)OC)OC)NC(=O)NC(C)(C)C | ||
Löslichkeit
|
In vitro |
DMSO
: 105 mg/mL
(200.5 mM)
Ethanol : 105 mg/mL Water : Insoluble |
Molaritätsrechner
Verdünnungsrechner
Molekulargewichtsrechner
|
In vivo |
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In-vivo-Formulierungsrechner (Klare Lösung)
Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)
mg/kg
g
μL
Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Berechnungsergebnisse:
Arbeitskonzentration: mg/ml;
Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )
Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH2O, mischen und klären.
Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.
Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.
Wirkmechanismus
| Targets/IC50/Ki |
FGFR1
(Cell-free assay) ~25 nM
VEGFR2
(Cell-free assay) 100 nM-200 nM
|
|---|---|
| In vitro |
PD173074 ist ein ATP-kompetitiver Inhibitor von FGFR1 mit einem Ki von ~40 nM. Diese Verbindung ist auch ein wirksamer Inhibitor von VEGFR2. Im Vergleich zu FGFR1 hemmt sie die Aktivitäten von Src, InsR, EGFR, PDGFR, MEK und PKC schwach mit 1000-fach oder höheren IC50-Werten. Dieser Inhibitor hemmt die Autophosphorylierung von FGFR1 und VEGFR2 dosisabhängig mit einer IC50 von 1-5 nM bzw. 100-200 nM. Er hemmt die FGF-2-Förderung des Überlebens von Granula-Neuronen dosisabhängig mit einer IC50 von 12 nM, wobei er eine 1.000-fach höhere Wirksamkeit als SU 5402 aufweist. Diese Chemikalie hemmt spezifisch FGF-2-vermittelte Effekte auf Proliferation, Differenzierung und MAPK-Aktivierung in Oligodendrozyten (OL)-Linienzellen. Sie ist aktiv gegen den WT-Rezeptor und FGFR3-Mutationen in Multiples Myelom (MM)-Zelllinien. Diese Verbindung hemmt auch potent die Autophosphorylierung von FGFR3 dosisabhängig mit einer IC50 von ~5 nM. Ihre Behandlung reduziert potent die Lebensfähigkeit von FGFR3-exprimierenden KMS11- und KMS18-Zellen mit einer IC50 von <20 nM. Die Hemmung des aFGF-stimulierten MM-Zellwachstums durch dieses Mittel korreliert stark mit der Expression von FGFR3. Ihre Behandlung hebt die NIH 3T3-Transformation, die durch Y373C FGFR3, aber nicht durch Ras V12 vermittelt wird, vollständig auf, was zeigt, dass sie spezifisch auf die FGFR3-vermittelte Zelltransformation abzielt und keine unspezifische zytotoxische Wirkung hat. Diese Chemikalie induziert auch die funktionelle Reifung von KMS11- und KMS18-Zellen.
|
| Kinase-Assay |
In-vitro-Kinase-Inhibitions-Assays
|
|
Assays unter Verwendung der vollständigen FGFR-1-Kinase werden in einem Gesamtvolumen von 100 μL durchgeführt, das 25 mM HEPES-Puffer (pH 7,4), 150 mM NaCl, 10 mM MnCl2, 0,2 mM Natriumorthovanadat, eine Konzentration von 750 μg/mL eines zufälligen Copolymers aus Glutaminsäure und Tyrosin (4:1), verschiedene Konzentrationen von PD173074 und 60 bis 75 ng Enzym enthält. Die Reaktion wird durch Zugabe von [γ-32P]ATP (5 μM ATP, das 0,4 μCi [γ-32P]ATP pro Inkubation enthält) eingeleitet, und die Proben werden 10 Minuten bei 25°C inkubiert. Die Reaktion wird durch Zugabe von 30 % Trichloressigsäure und die Fällung des Materials auf Glasfaserfiltermatten beendet. Die Filter werden dreimal mit 15 % Trichloressigsäure gewaschen, und der Einbau von [32P] in das Glutamat-Tyrosin-Polymer-Substrat wird durch Zählung der auf den Filtern verbleibenden Radioaktivität in einem Wallac 1250 Betaplate Reader bestimmt. Unspezifische Aktivität ist definiert als Radioaktivität, die auf den Filtern nach Inkubation von Proben ohne Enzym verbleibt. Spezifische Aktivität wird als Gesamtaktivität (Enzym plus Puffer) minus unspezifische Aktivität bestimmt. Die Konzentration dieser Verbindung, die die FGFR-1-Enzymaktivität um 50 % hemmt (IC50), wird grafisch bestimmt.
|
|
| In vivo |
Die Verabreichung von PD173074 in Dosen von 1 mg/kg/Tag oder 2 mg/kg/Tag an Mäuse kann die durch FGF oder VEGF induzierte Angiogenese dosisabhängig und ohne offensichtliche Toxizität wirksam blockieren. Diese Verbindung hemmt das In-vivo-Wachstum von mutant FGFR3-transfiziert NIH 3T3-Zellen in Nacktmäusen. Die Hemmung von FGFR3 durch diese Chemikalie verzögert das Tumorwachstum und erhöht das Überleben von Mäusen in einem KMS11-Xenograft-Myelommodell. Im H-510-Xenograft blockiert die orale Verabreichung dieser Verbindung das Tumorwachstum ähnlich wie bei einer Cisplatin-Einzeltherapie, wodurch das mittlere Überleben im Vergleich zu Kontrolltieren mit Scheineingriff verlängert wird. In H-69-Xenografts induziert diese Chemikalie bei 50 % der Mäuse vollständige Remissionen, die >6 Monate andauern. Diese Effekte korrelieren mit einer erhöhten Apoptose in exzidierten Tumoren, sind aber keine Folge einer gestörten Tumorgefäßversorgung.
|
Literatur |
|
Anwendungen
| Methoden | Biomarker | Bilder | 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 |
Technischer Support
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Wenn Sie weitere Fragen haben, hinterlassen Sie bitte eine Nachricht.
Häufig gestellte Fragen
Frage 1:
What is the half-life of this compound (S1264) in vivo?
Antwort:
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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