Chemical Structure : HMPL-453
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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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.
M.Wt | 509.05 | |
Formula | C27H33ClN6O2 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
1. Jia Hu, et al. Cancer Res (2023) 83 (7_Supplement): 6321.
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