General description
一种有效的、选择性的、不可逆的FGFR抑制剂，对FGFR1/2/3/4的IC50分别为3.09nM、4.3nM、27nM和45.3nM。
FIIN-2 is a potent, selective, irreversible and the next-generation covalent FGFR inhibitor. FIIN-2 is the first inhibitor that can potently inhibit the proliferation of cells dependent upon the gatekeeper mutants of FGFR1 or FGFR2, which confer resistance to first-generation clinical FGFR inhibitors such as NVP-BGJ398 and AZD4547. FIIN-2 also binds in the DFG-out mode despite lacking a functional group necessary to occupy the pocket vacated upon the DFG-out flip。
FIIN-2是一种有效的，选择性的，不可逆的下一代共价FGFR抑制剂。 FIIN-2是第一种可以有效抑制依赖于FGFR1或FGFR2的关守突变体的细胞增殖的抑制剂，这赋予了对第一代临床FGFR抑制剂（如NVP-BGJ398和AZD4547）的抗性。 尽管没有必要的功能基团来占据DFG-out翻转时腾出的口袋，但FIIN-2仍以DFG-out模式结合。
Properties
| Iupac Name： | N-(4-((3-(3,5-dimethoxyphenyl)-7-((4-(4-methylpiperazin-1-yl)phenyl)amino)-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl)methyl)phenyl)acrylamide |
| Inchi Code | 1S/C35H38N8O4/c1-5-32(44)37-26-8-6-24(7-9-26)22-43-33-25(23-42(35(43)45)29-18-30(46-3)20-31(19-29)47-4)21-36-34(39-33)38-27-10-12-28(13-11-27)41-16-14-40(2)15-17-41/h5-13,18-21H,1,14-17,22-23H2,2-4H3,(H,37,44)(H,36,38,39) |
| Inchi Key | DVBPRWJMHURKHP-UHFFFAOYSA-N |
安全信息
