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PD173074
PD173074 是一種有效的FGFR1抑制劑，在無細胞試驗中IC50約為25 nM，也能抑制VEGFR2，IC50為100-200 nM，作用于FGFR1比作用于PDGFR和c-Src選擇性高1000倍左右。PD173074 可在胃癌細胞中抑制增殖并促進凋亡。
PD173074 Chemical Structure
CAS: 219580-11-7
產(chǎn)品質(zhì)控
批次：
純度：
99.72%
99.72
PD173074相關(guān)產(chǎn)品
| 相關(guān)靶點 | FGFR1 FGFR2 FGFR3 FGFR4 | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | Fexagratinib (AZD4547) BLU9931 LY2874455 Zoligratinib (Debio-1347) Futibatinib (TAS-120) PD-166866 SSR128129E H3B-6527 Fisogatinib (BLU-554) Derazantinib FIIN-2 Ferulic Acid ASP5878 Roblitinib (FGF401) Alofanib (RPT835) NSC12 PRN1371 | 點擊展開 |
| 相關(guān)化合物庫 | 酪氨酸激酶抑制劑分子庫 PI3K/Akt 抑制劑庫 血管生成相關(guān)化合物庫 HIF-1信號通路化合物庫 FDA抗癌藥物庫 | 點擊展開 |
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 |
| 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 | |
| SK-MEL-30 | Growth Inhibition Assay | IC50=10.8901 μM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=10.7391 μM | SANGER | ||
| BE-13 | Growth Inhibition Assay | IC50=10.6576 μM | SANGER | ||
| OAW-42 | Growth Inhibition Assay | IC50=10.5267 μM | SANGER | ||
| SW948 | Growth Inhibition Assay | IC50=10.1882 μM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=10.1393 μM | SANGER | ||
| CAS-1 | Growth Inhibition Assay | IC50=9.97659 μM | SANGER | ||
| IST-MES1 | Growth Inhibition Assay | IC50=9.94534 μM | SANGER | ||
| EW-13 | Growth Inhibition Assay | IC50=9.89055 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=9.50595 μM | SANGER | ||
| HOS | Growth Inhibition Assay | IC50=9.35134 μM | SANGER | ||
| NCI-H446 | Growth Inhibition Assay | IC50=9.29526 μM | SANGER | ||
| DBTRG-05MG | Growth Inhibition Assay | IC50=9.09607 μM | SANGER | ||
| D-283MED | Growth Inhibition Assay | IC50=9.06534 μM | SANGER | ||
| TE-6 | Growth Inhibition Assay | IC50=8.75143 μM | SANGER | ||
| SW954 | Growth Inhibition Assay | IC50=8.69786 μM | SANGER | ||
| NCI-H520 | Growth Inhibition Assay | IC50=8.62157 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=8.52212 μM | SANGER | ||
| COR-L88 | Growth Inhibition Assay | IC50=8.50981 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=8.48149 μM | SANGER | ||
| DB | Growth Inhibition Assay | IC50=8.11504 μM | SANGER | ||
| ES8 | Growth Inhibition Assay | IC50=7.69626 μM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=7.48341 μM | SANGER | ||
| SK-MEL-28 | Growth Inhibition Assay | IC50=7.37819 μM | SANGER | ||
| ME-180 | Growth Inhibition Assay | IC50=7.10404 μM | SANGER | ||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=7.07764 μM | SANGER | ||
| SK-UT-1 | Growth Inhibition Assay | IC50=6.91784 μM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=6.76626 μM | SANGER | ||
| A4-Fuk | Growth Inhibition Assay | IC50=6.73142 μM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=6.72671 μM | SANGER | ||
| NCI-H1355 | Growth Inhibition Assay | IC50=6.41733 μM | SANGER | ||
| CHP-134 | Growth Inhibition Assay | IC50=6.25182 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=6.24977 μM | SANGER | ||
| SF126 | Growth Inhibition Assay | IC50=6.21406 μM | SANGER | ||
| NCI-H1770 | Growth Inhibition Assay | IC50=5.95032 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=5.72927 μM | SANGER | ||
| HuO9 | Growth Inhibition Assay | IC50=5.38843 μM | SANGER | ||
| SK-MEL-3 | Growth Inhibition Assay | IC50=5.2406 μM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=4.96665 μM | SANGER | ||
| IGROV-1 | Growth Inhibition Assay | IC50=4.87168 μM | SANGER | ||
| NCI-H209 | Growth Inhibition Assay | IC50=4.58283 μM | SANGER | ||
| KM-H2 | Growth Inhibition Assay | IC50=4.55222 μM | SANGER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=4.5481 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=4.5331 μM | SANGER | ||
| D-336MG | Growth Inhibition Assay | IC50=4.46817 μM | SANGER | ||
| CAL-72 | Growth Inhibition Assay | IC50=4.41746 μM | SANGER | ||
| LU-139 | Growth Inhibition Assay | IC50=4.31534 μM | SANGER | ||
| A704 | Growth Inhibition Assay | IC50=4.28723 μM | SANGER | ||
| EW-3 | Growth Inhibition Assay | IC50=3.98923 μM | SANGER | ||
| SW780 | Growth Inhibition Assay | IC50=3.92245 μM | SANGER | ||
| A204 | Growth Inhibition Assay | IC50=3.92075 μM | SANGER | ||
| ES5 | Growth Inhibition Assay | IC50=3.83637 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=3.80051 μM | SANGER | ||
| Hs-578-T | Growth Inhibition Assay | IC50=3.67873 μM | SANGER | ||
| LK-2 | Growth Inhibition Assay | IC50=3.67133 μM | SANGER | ||
| CHL-1 | Growth Inhibition Assay | IC50=3.65799 μM | SANGER | ||
| NBsusSR | Growth Inhibition Assay | IC50=3.63969 μM | SANGER | ||
| CCRF-CEM | Growth Inhibition Assay | IC50=3.50488 μM | SANGER | ||
| RO82-W-1 | Growth Inhibition Assay | IC50=3.49855 μM | SANGER | ||
| HH | Growth Inhibition Assay | IC50=3.47676 μM | SANGER | ||
| GAMG | Growth Inhibition Assay | IC50=3.46576 μM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=3.23447 μM | SANGER | ||
| NCI-H1092 | Growth Inhibition Assay | IC50=3.1969 μM | SANGER | ||
| RH-18 | Growth Inhibition Assay | IC50=3.19598 μM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=3.13564 μM | SANGER | ||
| G-402 | Growth Inhibition Assay | IC50=3.12727 μM | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=3.03472 μM | SANGER | ||
| MG-63 | Growth Inhibition Assay | IC50=2.94262 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=2.70747 μM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=2.65331 μM | SANGER | ||
| MPP-89 | Growth Inhibition Assay | IC50=2.48364 μM | SANGER | ||
| G-401 | Growth Inhibition Assay | IC50=2.47189 μM | SANGER | ||
| HCC2218 | Growth Inhibition Assay | IC50=2.37939 μM | SANGER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=2.21283 μM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=2.18394 μM | SANGER | ||
| H9 | Growth Inhibition Assay | IC50=2.14306 μM | SANGER | ||
| SBC-1 | Growth Inhibition Assay | IC50=2.094 μM | SANGER | ||
| A172 | Growth Inhibition Assay | IC50=1.70355 μM | SANGER | ||
| DU-145 | Growth Inhibition Assay | IC50=1.58217 μM | SANGER | ||
| MSTO-211H | Growth Inhibition Assay | IC50=1.47378 μM | SANGER | ||
| DMS-114 | Growth Inhibition Assay | IC50=1.36737 μM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=1.33886 μM | SANGER | ||
| HuH-7 | Growth Inhibition Assay | IC50=1.24464 μM | SANGER | ||
| MFE-280 | Growth Inhibition Assay | IC50=0.85872 μM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=0.84623 μM | SANGER | ||
| SW962 | Growth Inhibition Assay | IC50=0.78988 μM | SANGER | ||
| D-263MG | Growth Inhibition Assay | IC50=0.71159 μM | SANGER | ||
| NEC8 | Growth Inhibition Assay | IC50=0.56289 μM | SANGER | ||
| RT-112 | Growth Inhibition Assay | IC50=0.54701 μM | SANGER | ||
| HuO-3N1 | Growth Inhibition Assay | IC50=0.54653 μM | SANGER | ||
| AN3-CA | Growth Inhibition Assay | IC50=0.40133 μM | SANGER | ||
| H-EMC-SS | Growth Inhibition Assay | IC50=0.34715 μM | SANGER | ||
| ECC10 | Growth Inhibition Assay | IC50=0.33898 μM | SANGER | ||
| EoL-1-cell | Growth Inhibition Assay | IC50=0.32984 μM | SANGER | ||
| MFM-223 | Growth Inhibition Assay | IC50=0.21576 μM | SANGER | ||
| KG-1 | Growth Inhibition Assay | IC50=0.05129 μM | SANGER | ||
| NCI-H1581 | Growth Inhibition Assay | IC50=0.01225 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 | ||
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | PD173074 是一種有效的FGFR1抑制劑，在無細胞試驗中IC50約為25 nM，也能抑制VEGFR2，IC50為100-200 nM，作用于FGFR1比作用于PDGFR和c-Src選擇性高1000倍左右。PD173074 可在胃癌細胞中抑制增殖并促進凋亡。 | ||||
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| 靶點 |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | PD173074是FGFR1的ATP競爭性抑制劑， Ki約為40 nM。PD173074也是VEGFR2的有效抑制劑。相比FGFR1，PD173074弱抑制Src，INSR，EGFR，PDGFR，MEK和PKC的活性，IC 50值大1000倍以上。PD173074劑量依賴性地抑制FGFR1和VEGFR2的自身磷酸化，IC50 分別為1-5 nM和100-200 nM。[1] PD173074以劑量依賴的方式抑制FGF-2促進的顆粒神經(jīng)元存活，IC50是12 nM，活性是SU 5402的1,000倍以上。[2] D173074特異性地抑制FGF-2-介導(dǎo)的少突膠質(zhì)細胞（OL）譜系細胞的細胞增殖，分化和MAPK激活。[3] 在多發(fā)性骨髓瘤（MM）細胞系中，PD173074對野生受體和FGFR3突變有活性。PD173074還以劑量依賴的方式有效地抑制FGFR3的自磷酸化，IC50約為5 nM。PD173074有力地降低了表達FGFR3的KMS11細胞和KMS18細胞的活力，IC50小于20 nM。aFGF刺激的MM細胞生長受PD173074抑制是和FGFR3的表達高度相關(guān)的。PD173074完全抑制由Y373C FGFR3介導(dǎo)而不是的Ras介導(dǎo)的NIH 3T3轉(zhuǎn)化，這表明PD173074專門針對FGFR3基因介導(dǎo)的細胞轉(zhuǎn)化和缺乏非特異性的細胞毒性作用。PD173074也誘導(dǎo)KMS11和KMS18細胞功能成熟。[4] | |||
|---|---|---|---|---|
| 激酶實驗 | 體外激酶抑制試驗 | |||
| 檢測是使用全長FGFR-1激酶在100微升含25 mM HEPES緩沖液（pH7.4），150 mM氯化鈉，10 mM MnCl2，0.2 mM的原釩酸鈉，750 μg/mL谷氨酸和酪氨酸（4:1）的無規(guī)共聚物，各種濃度的PD173074，和60至75 ng酶中進行的。該反應(yīng)通過加入[γ-32P]ATP（含有0.4 μCi of [γ-32P]ATP的5 μM ATP）起始，樣品在25°C孵育10分鐘。反應(yīng)通過加入30％三氯乙酸和材料的沉淀到玻璃纖維濾墊上終止。過濾器用15％三氯乙酸洗滌三次，摻入[32P]到谷氨酸酪氨酸聚合物襯底是通過計算保留在過濾器上的放射性來確定，通過WALLAC1250 betaplate閱讀器讀取。非特異性的活性被定義為溫育不含酶的樣品保留在過濾器上放射性。特異活性被確定為總活性（酶加緩沖液）減去非特異性活性。PD173074抑制FGFR-1的酶活性的IC50濃度用圖解法測定。 | ||||
| 細胞實驗 | 細胞系 | KMS11和 KMS18 | ||
| 濃度 | 溶解在DMSO中至終濃度~100 nM | |||
| 孵育時間 | 48小時 | |||
| 方法 | 在aFGF/肝素的存在下，細胞在PD173074濃度梯度中孵育48小時?；罴毎陌俜直扔蒑TT法檢測。 | |||
| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Western blot | pFGFR2 / FGFR2 p-S6RP / p-PRAS40 / p-p105 NFKB / P105 NFKB / P50 NFKB / p-AMPK / p-CRK II / p-PDK1 |
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24968263 | |
| Growth inhibition assay | Cell viability |
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24968263 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | PD173074在1 mg/kg/day或2 mg/ka/day對小鼠給藥可以劑量依賴性的方式有效阻止由FGF或VEGF誘導(dǎo)的血管生成，并沒有明顯的毒性。[1] PD173074抑制FGFR3突變體轉(zhuǎn)染的NIH 3T3細胞在裸鼠體內(nèi)生長。在KMS11異種移植瘤模型中，PD173074抑制FGFR3導(dǎo)致腫瘤生長延緩，小鼠的存活率提高。[4] 在H-510異種移植體中，PD173074阻斷腫瘤生長和cisplatin相似，與對照假治療的動物相比增加中位生存期。在H-69異種移植體中，PD173074在50％小鼠中的誘導(dǎo)作用長于6個月。這些效應(yīng)是和切除腫瘤中增加的細胞凋亡相關(guān)的，而非破壞腫瘤血管。[5] | |
|---|---|---|
| 動物實驗 | Animal Models | 誘導(dǎo)角膜新生血管的瑞士韋伯斯特小鼠 |
| Dosages | 約2 mg/kg/day | |
| Administration | 腹腔注射 | |
化學(xué)信息&溶解度
| 分子量 | 523.67 | 分子式 | C28H41N7O3 |
| CAS號 | 219580-11-7 | SDF | Download PD173074 SDF |
| Smiles | CCN(CC)CCCCNC1=NC2=NC(=C(C=C2C=N1)C3=CC(=CC(=C3)OC)OC)NC(=O)NC(C)(C)C | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 100 mg/mL ( (190.95 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 100 mg/mL (190.95 mM) Water : Insoluble |
摩爾濃度計算器 |
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體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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常見問題及建議解決方法
問題 1:
What is the half-life of PD173074(S1264) in vivo?
回答：
According to literature research, PD173074 is given twice daily because it 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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