FGFR4-IN-5 - ≥98% , CAS No.1628793-01-0

CAS: 1628793-01-0 Cat. No.: F648921 Molecular Weight: 520.37

GRADE & PURITY ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Overview

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 research

In Vivo

FGFR4-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:Solid

IC50& Target:FGFR4 6.5 nM (IC 50 ) FGFR2 505 nM (IC 50 )

Specifications

Specifications & Purity

≥98%

Biochemical and Physiological Mechanisms

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 research.

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Purity

≥98%

Names and Identifiers

• Molecular Weight: 520.37

Chemical and Physical Properties

• Solubility: DMSO : 100 mg/mL (192.17 mM; Need ultrasonic)