Network Version
Capmatinib Data Sheet
| Product Name: | Capmatinib |
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|---|---|---|
| CAS No.: | 1029712-80-8 | |
| Cat. No.: | HY-13404 | |
| MWt: | 412.42 | |
| Formula: | C23H17FN6O | |
| Purity : | >98% | |
| Solubility: | H<sub>2</sub>O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C);DMSO : 5 mg/mL (ultrasonic;warming;heat to 60°C) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
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Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase[1][2][3].
IC50 & Target:IC50: 0.13 nM (c-MET)[1]
In Vitro:Capmatinib (INCB28060) inhibits c-MET phosphorylation with an IC50 value of approximately 1 nM and a concentration of approximately 4 nM inhibits c-MET more than 90%, which is reversible and the effect is significantly reduced in several hours after the compound is removed and completely disappeared by 48 hours[1]. Capmatinib (INCB28060) (0-10000 nM; 72 h) inhibits the proliferation of SNU-5, S114, H441 and U-87MG[1]. Capmatinib (INCB28060) (0.06-62.25 nM; 2h) effectively inhibits phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5[1]. Capmatinib (INCB28060) (0.24-63 nM; over night) prevents HGF-stimulated H441 cell migration[1]. Capmatinib (INCB28060) (0.5-50 nM; 20 min) suppresses phosphorylation of both EGFR and HER-3 rapidly[1]. Capmatinib (INCB28060) (0-333 nM; 24 h) induces apoptosis in SNU-5 cells[1]. In Vivo:Capmatinib (INCB28060) (1-30 mg/kg; PO, twice daily, for 2 weeks) exhibits dose-dependent inhibition of tumor growth, and shows well tolerance at all doses during the treatment periods, with no evidence of overt toxicity or weight loss in U-87MG tumor mice model[1]. Capmatinib (INCB28060) (0.03-10 mg/kg; PO, single dosage) causes inhibition of c-MET phosphorylation in S114 tumor mice model[1]. |
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