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HMPL-453

Chemical Structure : HMPL-453

CAS No.: 1628537-44-9

HMPL-453 (Fanregratinib, HMPL453)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 509.05
Formula C27H33ClN6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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

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