ChemicalBook CAS DataBase List 1029714-89-3

1029714-89-3

Name	INCB28060
CAS	1029714-89-3
Molecular Formula	C23H18ClFN6O
Molecular Weight	448.89
MOL File	1029714-89-3.mol

Chemical Properties

form	Solid
color	Off-white to light yellow

Hazard Information

Uses

Capmatinib (INC280; INCB28060) hydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib hydrochloride 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 hydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib hydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase[1][2][3].

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].

Animal Model:	Female Balb/c nu/nu mice (inoculated subcutaneously with 5×10⁶ U-87MG glioblastoma cells)^[1]
Dosage:	1, 3, 10 and 30 mg/kg
Administration:	PO, twice daily, for 2 weeks
Result:	Exhibited dose-dependent inhibition of tumor growth with 35% and 76% at 1 and 3 mg/kg once daily; resulted in partial regressions in 6 of 10 U-87MG tumor-bearing mice at 10 mg/kg once daily; and showed well tolerance at all doses during the treatment periods, with no evidence of overt toxicity or weight loss.

Animal Model:	Female Balb/c nu/nu mice (inoculated subcutaneously with 4×10⁶ S114 tumor cells)^[1]
Dosage:	0.03, 0.1, 0.3, 1, 3 and 10 mg/kg
Administration:	PO, single dosage
Result:	Caused approximately 50% and 90% inhibition of c-MET phosphorylation at 0.03 and 0.3 mg/kg after administration of 30 min, and inhibition of phospho-c-MET exceeded 90% after 7 hours.

References

[1] Liu X, et al. A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3. Clin Cancer Res. 2011 Nov 15;17(22):7127-38. DOI:10.1158/1078-0432.CCR-11-1157
[2] Baltschukat S, et al. Capmatinib (INC280) Is Active Against Models of Non-Small Cell Lung Cancer and Other Cancer Types with Defined Mechanisms of MET Activation. Clin Cancer Res. 2019 May 15;25(10):3164-3175. DOI:10.1158/1078-0432.CCR-18-2814
[3] Dhillon S. Capmatinib: First Approval. Drugs. 2020 Jul;80(11):1125-1131. DOI:10.1007/s40265-020-01347-3

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