HMPL-453 (Fanregratinib) | FGFR1/2/3 inhibitor | Probechem Biochemicals

Chemical Structure : HMPL-453

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HMPL-453 (Fanregratinib, HMPL453)

货号: PC-24953Not For Human Use, Lab Use Only.

HMPL-453 (Fanregratinib) is a potent, highly selective inhibitor of fibroblast growth factor receptors 1, 2, and 3 (FGFR1/2/3) with IC50 of 6, 4, and 6 nM, respectively, shows weaker activity against FGFR4 (IC50=425 nM).

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生物&药学活性

HMPL-453 (Fanregratinib) is a potent, highly selective inhibitor of fibroblast growth factor receptors 1, 2, and 3 (FGFR1/2/3) with IC50 of 6, 4, and 6 nM, respectively, shows weaker activity against FGFR4 (IC50=425 nM).
HMPL-453 selectively inhibits proliferation of tumor cell lines with dysregulated FGFR signaling with GI50 values of 3-105 nM, sparing cell lines lacking FGFR aberrations (GI50>1.5 uM).
HMPL-453 demonstrates strong inhibition of phosphorylation of FGFR and downstream protein in tumor cell lines harboring FGFR2 fusion.
HMPL-453 (50 mg/kg/day) could induce time- and dose-dependent inhibition of phosphorylation of FGFR and resulted in remarkable and dose-dependent anti-tumor activity in multiple FGFR-altered tumor models.

物理化学性质&存储条件

分子量	509.05
分子式	C27H33ClN6O2
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	4-chloro-3-(2-(2-((4-((3S,5R)-3,5-dimethylpiperazin-1-yl)phenyl)amino)pyrimidin-5-yl)ethyl)-5-methoxy-N-methylbenzamide

参考文献

1. Jia Hu, et al. Cancer Res (2023) 83 (7_Supplement): 6321.

HMPL-453 (Fanregratinib, HMPL453)

生物&药学活性

物理化学性质&存储条件

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HMPL-453 (Fanregratinib, HMPL453)

生物&药学活性

物理化学性质&存储条件

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