瑞格非尼
CAS号 | 755037-03-7 | 货号 | BCP02105 |
中文名 | 瑞格非尼 | ||
英文名 | Regorafenib | ||
中文别名 | |||
英文别名 | BAY 734506; BAY734506; BAY-734506;BAY 73-4506;BAY73-4506; | ||
分子式 | C21H15ClF4N4O3 | 分子量 | 482.82 |
生物活性 | Regorafenib strongly prevents VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with IC50 of 3 nM. In HAoSMCs, regorafenib suppress PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50 of 90 nM. Regorafenib also inhibits FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10. Regorafenib very potently inhibited the mutant receptors KITK642E and RETC634W, with IC50 of approximately 20 nM and 10 nM, respectively. Regorafenib inhibits the proliferation of VEGF165-stimulated HUVECs, with an IC50 of approximately 3 nM. Regorafenib prevents the proliferation of FGF2-stimulated HUVECs and of PDGF-BB-stimulated HAoSMCs with IC50 of 127 nM and 146 nM, respectively. | ||
上下游产品 | 1019206-88-2(瑞格非尼(一水合物)) 835621-07-3(盐酸瑞格非尼) | ||
信号通路 | Angiogenesis/Protein Tyrosine Kinase MAPK Pathway | ||
靶 点 | PDGFR VEGFR c Kit RET Raf |
结构式
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