FIIN-3 is a potent, selective, irreversible and the next-generation covalent FGFR inhibitor. FIIN-3 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-3 has the unprecedented ability to inhibit both the EGF receptor (EGFR) and FGFR covalently by targeting two distinct cysteine residues. FIIN-3 bound with FGFR4 V550L and EGFR L858R. (Proc Natl Acad Sci U S A. 2014 Nov 11;111(45):E4869-77.)
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化学信息
名称 | FIIN-3 |
Iupac 化学名称 | FIIN-3 |
同义词 | FIIN3; FIIN 3 |
英文同义词 | FIIN3; FIIN 3 |
分子式 | C34H36Cl2N8O4 |
分子量 | 691.60684 |
InChiKey | |
InChi | |
Cas号 | 1637735-84-2 |
相关CAS号 | |
外观性状 | crystalline solid |
纯度 | 98% |
存储 | 3 years -20ºCpowder |
可溶性 | Soluble in DMSO |
处理方式 | |
运输条件 | Shipped under ambient temperature as non-hazardous chemical. |
海关编码 | |
Targets | |
Mechanism | |
Cell study | |
Animal study | |
Clinical study | |