Powder: -20°C for 3 years | In solvent: -80°C for 1 year
FGFR4-IN-5, a covalent FGFR4 inhibitor, demonstrates potency and selectivity with an IC50 value of 6.5 nM. Exhibiting significant in vivo anti-tumor activity, it is applicable for research in hepatocellular carcinoma [1].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 1,670.00 | |
50 mg | 6-8 weeks | $ 2,180.00 | |
100 mg | 6-8 weeks | $ 2,800.00 |
Description | FGFR4-IN-5, a covalent FGFR4 inhibitor, demonstrates potency and selectivity with an IC50 value of 6.5 nM. Exhibiting significant in vivo anti-tumor activity, it is applicable for research in hepatocellular carcinoma [1]. |
Targets&IC50 | 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]. |
Synonyms | FGFR4-IN-5 |
Molecular Weight | 520.37 |
Formula | C23H23Cl2N5O5 |
CAS No. | 1628793-01-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (192.17 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. More
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FGFR4-IN-5 1628793-01-0 FGFR4 IN 5 FGFR-4-IN-5 FGFR4IN5 inhibitor inhibit