FGFRs-IN-1 (Compound A16) is the orally active inhibitor for FGFR, that inhibits FGFR1/2/3/4 with IC50s of 2.3, 7, 11, and 163 nM, respectively. FGFRs-IN-1 also inhibits VEGFR1/2/3, Abl, and Flt3 with IC50s of 61, 176, 112, 26, and 353 nM, respectively. FGFRs-IN-1 exhibits weak inhibitory efficacy against CYP enzymes. FGFRs-IN-1 reduces the expression of alpha-SMA and collagen I, and inhibits epithelial-mesenchymal transition (EMT) in TGF-beta1 stimulated A549 cell. FGFRs-IN-1 exhibits anti-inflammatory activity in Bleomycin (HY-17565)-induced mouse pulmonary fibrosis model and CCl4 (HY-Y0298)-induced mouse liver fibrosis model[1].
Molecular Weight:
537.44
Formula:
C28H26Cl2N4O3
Target:
Bcr-Abl,Cytochrome P450,FGFR,FLT3,VEGFR
Application Notes:
MCE Product type: Reference compound1
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