Chemical Structure : KNT-0919
CAS No.:
3067338-77-3
KNT-0919
(KNT0919)
Catalog No.: PC-26972Not For Human Use, Lab Use Only.
KNT-0919 is a potent, selective and covalent FGFR2/3 inhibitor, potently suppresses FGFR2- and FGFR3-driven Ba/F3 cells with IC50 of 1.1 nM and 0.20 nM respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
KNT-0919 is a potent, selective and covalent FGFR2/3 inhibitor, potently suppresses FGFR2- and FGFR3-driven Ba/F3 cells with IC50 of 1.1 nM and 0.20 nM respectively.
KNT-0919 displays much weaker or no activities against Ba/F3-FGFR1 cells (IC50=17.1 nM), Ba/F3-FGFR4 cells (IC50=228 nM) and parental Ba/F3 cells (IC50>1000 nM).
KNT-0919 selectively inhibits FGFR2/3 kinases, including clinically relevant mutants, in a panel of 416 kinases.
KNT-0919 selectively suppressed the proliferation of FGFR2-dependent cancer cell lines, dose-dependently inhibited FGFR2 downstream signaling, and induced apoptosis in an FGFR2-dependent manner.
KNT-0919 demonstrated favorable oral bioavailability (56%) in rats and achieved significant tumor growth inhibition in an SNU-16 gastric cancer xenograft model.
Physicochemical Properties
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M.Wt
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490.53
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Formula
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C25H20F2N6OS
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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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(R)-1-(4-amino-5-((2-cyclopropyl-4,6-difluorobenzo[d]thiazol-5-yl)ethynyl)-8-methyl-8,9-dihydropyrazino[1',2':1,5]pyrrolo[2,3-d]pyrimidin-7(6H)-yl)prop-2-en-1-one
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References
1. Lu X, et al. J Med Chem. 2026 Jun 8. doi: 10.1021/acs.jmedchem.6c00585.
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