FGFRs-IN-1
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 α-SMA and collagen I, and inhibits epithelial-mesenchymal transition (EMT) in TGF-β1 stimulated A549 cell. FGFRs-IN-1 exhibits anti-inflammatory activity in Bleomycin -induced mouse pulmonary fibrosis model and CCl4 (HY-Y0298) -induced mouse liver fibrosis model[1].
Product Specifications
UNSPSC
12352005
Target
Bcr-Abl; Cytochrome P450; FGFR; FLT3; VEGFR
Related Pathways
Metabolic Enzyme/Protease; Protein Tyrosine Kinase/RTK
Field of Research
Inflammation/Immunology
Smiles
O=C(C1=CC=C(/C=C/C2=NNC3=C2C=CC(C4=C(Cl)C(OC)=CC(OC)=C4Cl)=C3)C=C1)N5CCNCC5
Molecular Formula
C28H26Cl2N4O3
Molecular Weight
537.44
References & Citations
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Abl; CYP1A2; CYP2C19; CYP2D6; VEGFR1/Flt-1; VEGFR2/KDR/Flk-1; VEGFR3/Flt-4
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