Product Name

Capmatinib (INCB28060)

General description

Capmatinib is a novel, ATP-competitive inhibitor of c-MET.

Synonym

2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide; INC280, NVP-INC280

Purity

≥98.0%(HPLC)

CAS Number

1029712-80-8

Formula

C²³H¹⁷FN⁶O

Molecular Weight

412.42

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

solid

Solubility(25℃)

DMSO

Slightly soluble

Ethanol

Insoluble

Water

Insoluble

l  Biological Information

Biochem/Physiol  Actions

Capmatinib is an orally bioavailable inhibitor of the proto-oncogene c-Met (also known as hepatocyte growth factor receptor (HGFR)) with potential antineoplastic activity. Capmatinib selectively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways. This may induce cell death in tumor cells overexpressing c-Met protein or expressing constitutively activated c-Met protein. c-Met, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays key roles in tumor cell proliferation, survival, invasion, metastasis, and tumor angiogenesis.

Capmatinib is a novel, ATP-competitive inhibitor of c-MET with IC50 of 0.13 nM in a cell-free assay, inactive against RONβ, as well as EGFR and HER-3.

Application

Capmatinib has been used in trials studying the treatment of Melanoma, Gliosarcoma, Solid Tumors, Colorectal Cancer, and Hepatic Impairment, among others.

l  Storage

Storage temp.

-20℃

l  Precautions and Disclaimer

This product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov