FGFR4-IN-5 (C007B-355969)

FGFR4-IN-5 is a potent and selective covalent FGFR4 inhibitor with an IC 50 of 6.5 nM. FGFR4-IN-5 exhibits strong anti-tumor activity in vivo and can be used for hepatocellular carcinoma researchIn VivoFGFR4-IN-5 (oral gavage; 10 mg/kg; single dose) reveals a high C max , low clearance, the C max 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 . FGFR4-IN-5 (oral gavage; 100 mg/kg; twice daily; 28 days) exhibits strong antitumor activity in an orthotopic Hep3B HTX model . 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Hep3B cell bearing mice model 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 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.Form:SolidIC50& Target:FGFR4 6.5 nM (IC 50 ) FGFR2 505 nM (IC 50 ). Specification: 0.98 Molecular Formula: C23H23Cl2N5O5 Molecular Weight: 520.37

UPC:

51181614

Condition:

New

Weight:

1.06 Ounces

HazmatClass:

No

Quantity:

1

Unit of Measurement:

EA

WeightUOM:

LB

MPN:

F648921-10mg

CAS:

1628793-01-0

Product Size:

10mg