PD173074
PD173074 是一种有效的FGFR1抑制剂，在无细胞试验中IC50约为25 nM，也能抑制VEGFR2，IC50为100-200 nM，作用于FGFR1比作用于PDGFR和c-Src选择性高1000倍左右。PD173074 可在胃癌细胞中抑制增殖并促进凋亡。
PD173074 Chemical Structure
CAS: 219580-11-7
产品质控
批次：
纯度：
99.72%
99.72
PD173074相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
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生物活性
| 产品描述 | PD173074 是一种有效的FGFR1抑制剂，在无细胞试验中IC50约为25 nM，也能抑制VEGFR2，IC50为100-200 nM，作用于FGFR1比作用于PDGFR和c-Src选择性高1000倍左右。PD173074 可在胃癌细胞中抑制增殖并促进凋亡。 | ||||
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| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | PD173074是FGFR1的ATP竞争性抑制剂， Ki约为40 nM。PD173074也是VEGFR2的有效抑制剂。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剂量依赖性地抑制FGFR1和VEGFR2的自身磷酸化，IC50 分别为1-5 nM和100-200 nM。[1] PD173074以剂量依赖的方式抑制FGF-2促进的颗粒神经元存活，IC50是12 nM，活性是SU 5402的1,000倍以上。[2] D173074特异性地抑制FGF-2-介导的少突胶质细胞（OL）谱系细胞的细胞增殖，分化和MAPK激活。[3] 在多发性骨髓瘤（MM）细胞系中，PD173074对野生受体和FGFR3突变有活性。PD173074还以剂量依赖的方式有效地抑制FGFR3的自磷酸化，IC50约为5 nM。PD173074有力地降低了表达FGFR3的KMS11细胞和KMS18细胞的活力，IC50小于20 nM。aFGF刺激的MM细胞生长受PD173074抑制是和FGFR3的表达高度相关的。PD173074完全抑制由Y373C FGFR3介导而不是的Ras介导的NIH 3T3转化，这表明PD173074专门针对FGFR3基因介导的细胞转化和缺乏非特异性的细胞毒性作用。PD173074也诱导KMS11和KMS18细胞功能成熟。[4] | |||
|---|---|---|---|---|
| 激酶实验 | 体外激酶抑制试验 | |||
| 检测是使用全长FGFR-1激酶在100微升含25 mM HEPES缓冲液（pH7.4），150 mM氯化钠，10 mM MnCl2，0.2 mM的原钒酸钠，750 μg/mL谷氨酸和酪氨酸（4:1）的无规共聚物，各种浓度的PD173074，和60至75 ng酶中进行的。该反应通过加入[γ-32P]ATP（含有0.4 μCi of [γ-32P]ATP的5 μM ATP）起始，样品在25°C孵育10分钟。反应通过加入30％三氯乙酸和材料的沉淀到玻璃纤维滤垫上终止。过滤器用15％三氯乙酸洗涤三次，掺入[32P]到谷氨酸酪氨酸聚合物衬底是通过计算保留在过滤器上的放射性来确定，通过WALLAC1250 betaplate阅读器读取。非特异性的活性被定义为温育不含酶的样品保留在过滤器上放射性。特异活性被确定为总活性（酶加缓冲液）减去非特异性活性。PD173074抑制FGFR-1的酶活性的IC50浓度用图解法测定。 | ||||
| 细胞实验 | 细胞系 | KMS11和 KMS18 | ||
| 浓度 | 溶解在DMSO中至终浓度~100 nM | |||
| 孵育时间 | 48小时 | |||
| 方法 | 在aFGF/肝素的存在下，细胞在PD173074浓度梯度中孵育48小时。活细胞的百分比由MTT法检测。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | 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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| Growth inhibition assay | Cell viability |
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| 体内研究(In Vivo) | ||
| 体内研究活性 | PD173074在1 mg/kg/day或2 mg/ka/day对小鼠给药可以剂量依赖性的方式有效阻止由FGF或VEGF诱导的血管生成，并没有明显的毒性。[1] PD173074抑制FGFR3突变体转染的NIH 3T3细胞在裸鼠体内生长。在KMS11异种移植瘤模型中，PD173074抑制FGFR3导致肿瘤生长延缓，小鼠的存活率提高。[4] 在H-510异种移植体中，PD173074阻断肿瘤生长和cisplatin相似，与对照假治疗的动物相比增加中位生存期。在H-69异种移植体中，PD173074在50％小鼠中的诱导作用长于6个月。这些效应是和切除肿瘤中增加的细胞凋亡相关的，而非破坏肿瘤血管。[5] | |
|---|---|---|
| 动物实验 | Animal Models | 诱导角膜新生血管的瑞士韦伯斯特小鼠 |
| Dosages | 约2 mg/kg/day | |
| Administration | 腹腔注射 | |
化学信息&溶解度
| 分子量 | 523.67 | 分子式 | C28H41N7O3 |
| CAS号 | 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 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 100 mg/mL ( (190.95 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 100 mg/mL (190.95 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解配方 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | |||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 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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