1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. FGFR4-IN-5

FGFR4-IN-5 

Cat. No.: HY-131704
Handling Instructions

FGFR4-IN-5 is a potent and selective covalent FGFR4 inhibitor with an IC50 of 6.5 nM. FGFR4-IN-5 exhibits strong anti-tumor activity in vivo and can be used for hepatocellular carcinoma research.

For research use only. We do not sell to patients.

FGFR4-IN-5 Chemical Structure

FGFR4-IN-5 Chemical Structure

CAS No. : 1628793-01-0

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Description

FGFR4-IN-5 is a potent and selective covalent FGFR4 inhibitor with an IC50 of 6.5 nM. FGFR4-IN-5 exhibits strong anti-tumor activity in vivo and can be used for hepatocellular carcinoma research[1].

IC50 & Target[1]

FGFR4

6.5 nM (IC50)

FGFR2

505 nM (IC50)

In Vivo

FGFR4-IN-5 (oral gavage; 10 mg/kg; single dose) reveals a high Cmax, low clearance, the Cmax values are 423 ng/ml, 588 ng/ml, and 2820 ng/ml in mice, rat and cynamolgus monkey, respectively. And the oral bioavailability are 20, 12, and 27% in mouse, rat, and cyno, respectively[1].
FGFR4-IN-5 (oral gavage; 100 mg/kg; twice daily; 28 days) exhibits strong antitumor activity in an orthotopic Hep3B HTX model[1].
FGFR4-IN-5 (oral gavage; 10, 30, and 100 mg/kg; twice daily; 11 days) results in dose-dependent growth inhibition of resistant tumors. Tumor regression is observed at 30 and 100 mg/kg, with %ΔT/ΔC of 67% and 70%, respectively. However, treatment with sorafenib at 100 mg/kg once daily does not provide any benefit in vivo[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Hep3B cell bearing mice model[1]
Dosage: 100 mg/kg
Administration: Oral gavage; 100 mg/kg; twice daily; 28 days
Result: Resulted in tumor regression and sustained growth inhibition.
Animal Model: Sorafenib-resistant tumors established to mice bearing Huh7 tumors[1]
Dosage: 10, 30, and 100 mg/kg
Administration: Oral gavage; 10, 30, and 100 mg/kg; twice daily; 11 days
Result: Resulted in dose-dependent growth inhibition of resistant tumors.
Molecular Weight

520.37

Formula

C₂₃H₂₃Cl₂N₅O₅

CAS No.
SMILES

CN1C2=NC(N[[email protected]@H]3COC[[email protected]@H]3NC(C=C)=O)=NC=C2C=C(C4=C(Cl)C(OC)=CC(OC)=C4Cl)C1=O

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

FGFR4-IN-5FGFRFibroblast growth factor receptorFGF19-FGFR4HepatocellularcarcinomaHCCpFGFR4targeted covalentInhibitorinhibitorinhibit

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FGFR4-IN-5
Cat. No.:
HY-131704
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