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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 | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,670 | 6-8 weeks | 6-8 weeks | |
| 50 mg | $2,180 | 6-8 weeks | 6-8 weeks | |
| 100 mg | $2,800 | 6-8 weeks | 6-8 weeks |
| 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, administered via oral gavage at 10 mg/kg (single dose), shows high Cmax and low clearance, with Cmax values of 423 ng/ml in mice, 588 ng/ml in rats, and 2820 ng/ml in cynomolgus monkeys, and oral bioavailability of 20%, 12%, and 27%, respectively [1]. FGFR4-IN-5 (oral gavage; 100 mg/kg; twice daily; 28 days) demonstrates significant antitumor activity in an orthotopic Hep3B HTX model [1]. FGFR4-IN-5 (oral gavage; 10, 30, and 100 mg/kg; twice daily; 11 days) induces dose-dependent tumor growth inhibition, with regression at 30 and 100 mg/kg and %δT/δC values of 67% and 70%, respectively, while sorafenib (100 mg/kg; once daily) shows no in vivo benefit [1]. |
| Synonyms | FGFR4-IN-5 |
| Molecular Weight | 520.37 |
| Formula | C23H23Cl2N5O5 |
| Cas No. | 1628793-01-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (192.17 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (6.34 mM), Sonication is recommeded. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
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DMSO
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