CXF-009 | FGFR4 inhibitor | Probechem Biochemicals

Chemical Structure : CXF-009

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CXF-009 (CXF009)

货号: PC-73227Not For Human Use, Lab Use Only.

CXF-009 is a potent, specific, dual-warhead covalent inhibitor of FGFR4 (IC50=48 nM), forms dual-warhead covalent bonds with two cysteine residues in FGFR4.

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生物&药学活性

CXF-009 is a potent, specific, dual-warhead covalent inhibitor of FGFR4 (IC50=48 nM), forms dual-warhead covalent bonds with two cysteine residues in FGFR4.
CXF-009 forms covalent bonds with FGFR4(C477A) and FGFR4(C552A), respectively; display weak inhibition against FGFR1-3 with IC50 of 2579 nM, 2408 nM, and 977 nM.
CXF-009 shows inhibitory effect agaginst FGFR4 muntants FGFR4(C477A), FGFR4(C552A), and FGFR4(C477A, C552A) with IC50 of 193 nM, 602 nM, and 1528 nM, respectively.
CXF-009 inhibited the growth of Ba/F3 cells transformed with FGFR1-4 with IC50 values of 1562 nM, 1971 nM, 777 nM, and 38 nM, respectively.
CXF-009 is slightly more reactive to GSH than PRN1371.

物理化学性质&存储条件

分子量	626.718
分子式	C33H38N8O5
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	N-(2-((8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(3,5-dimethoxyphenyl)-7-oxo-5,6,7,8-tetrahydropyrimido[4,5-d]pyrimidin-2-yl)amino)phenyl)acrylamide

参考文献

1. Xiaojuan Chen, et al. Structure-based design of a dual-warhead covalent inhibitor of FGFR4. Commun Chem. 2022;5(1):36. Published 2022 Mar 17.

CXF-009 (CXF009)

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物理化学性质&存储条件

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CXF-009 (CXF009)

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