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首页-小分子抑制剂&激动剂-Tyrosine Kinase-FGFR-KNT-0919
KNT-0919

Chemical Structure : KNT-0919

CAS No.: 3067338-77-3

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KNT-0919 (KNT0919)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 490.53
分子式 C25H20F2N6OS
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

(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

参考文献

1. Lu X, et al. J Med Chem. 2026 Jun 8. doi: 10.1021/acs.jmedchem.6c00585.

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