2. Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease
  3. FGFR VEGFR Bcr-Abl FLT3 Cytochrome P450
  4. 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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FGFRs-IN-1 Chemical Structure

FGFRs-IN-1 Chemical Structure

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FGFRs-IN-1 Related Antibodies

Top Publications Citing Use of Products

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

View All Cytochrome P450 Isoform Specific Products:

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

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Description

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[1].

IC50 & Target

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)

Molecular Weight

537.44

Formula

C28H26Cl2N4O3
SMILES

O=C(C1=CC=C(/C=C/C2=NNC3=C2C=CC(C4=C(Cl)C(OC)=CC(OC)=C4Cl)=C3)C=C1)N5CCNCC5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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FGFRs-IN-1 Related Classifications

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The dilution calculator equation

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FGFRs-IN-1FGFRVEGFRBcr-AblFLT3Cytochrome P450Fibroblast growth factor receptorVascular endothelial growth factor receptorCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3CYPsorally activepulmonary fibrosisliver fibrosis,anti-fibroticA549Inhibitorinhibitorinhibit

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HY-170846
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