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首页-小分子抑制剂&激动剂-Tyrosine Kinase-FGFR-LHQ490
LHQ490

Chemical Structure : LHQ490

CAS No.: 3066470-16-1

LHQ490 (LHQ-490)

货号: PC-22316Not For Human Use, Lab Use Only.

LHQ490 is a potent, highly selective fibroblast growth factor receptor 2 (FGFR2) inhibitor with Ic50 of 5.2 nM, >61-, >34-, and >293-fold selective against FGFR1, FGFR3, and FGFR4.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

LHQ490 is a potent, highly selective fibroblast growth factor receptor 2 (FGFR2) inhibitor with Ic50 of 5.2 nM, >61-, >34-, and >293-fold selective against FGFR1, FGFR3, and FGFR4.
LHQ490 also exhibits high selectivity in a panel of 416 kinases.
LHQ490 efficiently suppresses the proliferation of BaF3-FGFR2 cells with IC50 of 1.4 nM, and displays >70- and >714-fold selectivity against BaF3-FGFR1 and the parental BaF3 cells, respectively.
LHQ490 potently suppresses the FGFR2 signaling pathways, selectively inhibits FGFR2-driven cancer cell proliferation, and induces apoptosis of FGFR2-driven cancer cells.

物理化学性质&存储条件

分子量 528.63
分子式 C30H33FN6O2
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

N-(4-(4-Amino-5-(4-(3-(ethyl(isopropyl)amino)oxetan-3-yl)-3-fluorophenyl)-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl)phenyl)acrylamide

参考文献

1. Huiqiong Li, et al. Eur J Med Chem. 2024 May 4:272:116473.

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