Cat. No. Name Size Price Add Cart
KI0632INCB2806010 mg$272
INCB2806050 mg$912

Chemical Characteristic

Product NameINCB28060
SynonymsIncyte
CAS No.1029712-80-8
Molecular Weight 412.42
FormulaC23H17FN6O
Chemical Name2-Fluoro-N-methyl-4-[7-[(quinolin-6-yl)methyl]imidazo[1,2-b]-[1,2,4]triazin-2-yl]benzamide
SmilesC(=O)(c1c(cc(cc1)c1nn2c(nc1)ncc2Cc1cc2cccnc2cc1)F)NC
Chemical Structure

Biological activities

INCB28060 is a novel inhibitor of c-MET kinase. INCB28060 inhibits c-MET kinase activity with an IC50 of 0.13 nM. INCB28060 inhibits SNU-5 proliferation with an IC50 of 1.2 nM and an IC90 of 4.6 nM. INCB28060 inhibits S114 cell proliferation with an IC50 of 12.4 nM. INCB28060 is highly active in U-87MG and H441 cells, with IC50 of 2.0 and 0.5 nM, respectively. INCB28060 prevents hepatocyte growth factor (HGF)-stimulated H441 cell migration, with an IC50 of 2.0 nM. INCB28060 effectively inhibits c-MET activation and signaling in cancer cells (SNU-5 human gastric cancer cell). Oral dosing of INCB28060 results in time- and dose-dependent inhibition of c-MET phosphorylation and tumor growth in c-MET-driven mouse tumor models.[1]

Protocols

INCB28060 is prepared as a 5 mM stock solution in 100% DMSO and routinely stored at room temperature. [1]

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, 17(22): 7127-7138.

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