Chemical Structure : CXF-009
Catalog No.: 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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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.
M.Wt | 626.718 | |
Formula | C33H38N8O5 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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.
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