Product Data Sheet

FGFR4-IN-8

Catalog No. A33566

main product photo
FGFR4-IN-8 is an ATP-competitive covalent inhibitor targeting fibroblast growth factor receptor 4 (FGFR4). It demonstrates potent activity against both wild-type FGFR4 and its gatekeeper mutants, with IC50 values of 0.5 nM for FGFR4, 0.25 nM for FGFR4V550L, 1.6 nM for FGFR4V550M, and 931 nM for FGFR4C552S. In addition, FGFR4-IN-8 exhibits significant antiproliferative effects on Hep3B hepatocellular carcinoma cells, with an IC50 of 29 nM, and shows modest antitumor efficacy in vivo in the Huh-7 xenograft mouse model, making it a valuable tool for cancer research.
Chemical Information
Catalog NumA33566
M. Wt654.56
FormulaC32H34Cl2FN7O3
Purity>98%
Storageat -20 °C 3 years (powder form); at -20 °C 6 months (Solution base)
CAS No.2765240-52-4
Synonyms
SMILESC[C@@H](OC1=CC=C(C2=C1)NN=C2NC3=C(C=C(C=C3F)N4CCC(CC4)N5CCOCC5)NC(C=C)=O)C6=C(C=NC=C6Cl)Cl
Biological Activity
DescriptionFGFR4-IN-8 is an ATP-competitive covalent inhibitor targeting fibroblast growth factor receptor 4 (FGFR4). It demonstrates potent activity against both wild-type FGFR4 and its gatekeeper mutants, with IC50 values of 0.5 nM for FGFR4, 0.25 nM for FGFR4V550L, 1.6 nM for FGFR4V550M, and 931 nM for FGFR4C552S. In addition, FGFR4-IN-8 exhibits significant antiproliferative effects on Hep3B hepatocellular carcinoma cells, with an IC50 of 29 nM, and shows modest antitumor efficacy in vivo in the Huh-7 xenograft mouse model, making it a valuable tool for cancer research.
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