Chemical Structure : CXF-007
CAS No.:
2727083-99-8
CXF-007
(CXF007)
Catalog No.: PC-28538Not For Human Use, Lab Use Only.
CXF-007 is a potent, selective covalent inhibitor of FGFR4 with IC50 of 7 nM, shows much weaker activity against FGFR1-3 with IC50 of 150-400 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
CXF-007 is a potent, selective covalent inhibitor of FGFR4 with IC50 of 7 nM, shows much weaker activity against FGFR1-3 with IC50 of 150-400 nM.
CXF-007 has IC50 of 530 nM, 445 nM, 170 nM and 1 nM for FGFR1/2/3/4 in Ba/F3 cells in Ba/F3 cell-viability assays, respectively.
CXF-007 potentially overcomes FGFR4 cysteine mutants, exhibits high activity against mutants against FGFR4(C477A), FGFR4(C552A) and FGFR4(C477A, C552A) with IC50 of 29 nM, 113 nM and 205 nM, respectively.
CXF-007 forms covalent bonds with Cys552 of FGFR4.
CXF-007 potently inhibits proliferation and FGFR4 signaling in cancer cell lines with abnormal FGFR4 expression (MDA-MB-453, IC50=0.37 uM).
Physicochemical Properties
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M.Wt
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619.68
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Formula
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C34H33N7O5
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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-(2-((8-(4-acrylamidophenethyl)-6-(3,5-dimethoxyphenyl)-7-oxo-5,6,7,8-tetrahydropyrimido [4,5-d] pyrimidin-2-yl) amino) phenyl) acrylamide
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References
1. Xiaojuan Chen, et al. Eur J Med Chem. 2024 Mar 15:268:116281.
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