Chemical Structure : LHQ490
CAS No.:
3066470-16-1
LHQ490
(LHQ-490)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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528.63
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Formula
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C30H33FN6O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Huiqiong Li, et al. Eur J Med Chem. 2024 May 4:272:116473.
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