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 (HY-17565)-induced mouse pulmonary fibrosis model and CCl4 (HY-Y0298)-induced mouse liver fibrosis model.
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- Formule: C28H26Cl2N4O3
- Masse moléculaire:537.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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FGFR1 2.3 nM (IC50) |
FGFR2 7 nM (IC50) |
FGFR3 11 nM (IC50) |
Abl 26 nM (IC50) |
Flt-1 61 nM (IC50) |
Flt-4 112 nM (IC50) |
FGFR4 163 nM (IC50) |
KDR 176 nM (IC50) |
Flt3 353 nM (IC50) |
CYP2D6 9.27 μM (IC50) |
CYP2C19 11.46 μM (IC50) |
CYP1A2 26.33 μM (IC50) |
Chemical Information
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Masse moléculaire 537.44
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Formule C28H26Cl2N4O3
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SMILES
O=C(C1=CC=C(/C=C/C2=NNC3=C2C=CC(C4=C(Cl)C(OC)=CC(OC)=C4Cl)=C3)C=C1)N5CCNCC5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FGFRs-IN-1 Related Classifications
HY-170846 Related Classifications
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