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首页-小分子抑制剂&激动剂-Tyrosine Kinase-FGFR-ISM7594
ISM7594

Chemical Structure : ISM7594

CAS No.: 3025799-76-9

ISM7594 (ISM-7594)

货号: PC-24856Not For Human Use, Lab Use Only.

ISM7594 is a potent, selective and covalent FGFR2/3 inhibitor with IC50 of 1.4/12.7 nM respectively, inhibits FGFR2 mutants and FGFR3 mutants with IC50 of 0.22-5.9 nM and 3.7-26 nM, selectively spares FGFR1/4.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ISM7594 is a potent, selective and covalent FGFR2/3 inhibitor with IC50 of 1.4/12.7 nM respectively, inhibits FGFR2 mutants and FGFR3 mutants with IC50 of 0.22-5.9 nM and 3.7-26 nM, selectively spares FGFR1/4.
ISM7594 exhibits robust suppression of both p-FGFR2 and p-ERK, with IC50 values of 1.5 and 2.1 nM, respectively, in SNU-16 cell line, exhibits antiproliferative IC50 of 1.6 nM.
ISM7594 demonstrates dual antiproliferation with average IC50 values of 4.5 and 7.3 nM against FGFR2- and FGFR3-altered cancer cells, respectively.
ISM7594 (30-60 mpk, BID) exhibits antitumor efficacy in 21-day SNU-16/RT4 xenograft models in Balb/c nude mice.

物理化学性质&存储条件

分子量 540.53
分子式 C29H22F2N6O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-(3-Fluoro-4-((4-methylpyrimidin-2-yl)oxy)phenyl)-7-(4-(2-fluoroacrylamido)phenyl)-3-methylpyrrolo[1,2-b]pyridazine-5-carboxamide

参考文献

1. Yazhou Wang, et al. J Med Chem. 2025 Jun 25. doi: 10.1021/acs.jmedchem.5c00928.

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