Cat No.
CEI-0833
Description
INCB28060 is a novel, ATP-competitive inhibitor of c-MET with IC50 of 0.13 nM, inactive against RONβ, as well as EGFR and HER-3. Phase 1.
CAS No.
1029712-80-8
IC50
0.13 nM
Targets
c-MET
Chemical Name
2-fluoro-N-methyl-4-(7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl)benzamide
M.Wt
412.42
Solubility
DMSO 2 mg/mL; Water <1 mg/mL; Ethanol <1 mg/mL
Storage
2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO.
In vitro
INCB28060 exhibits picomolar enzymatic potency and is highly specific for c-MET with more than 10,000-fold selectivity over a large panel of human kinases. INCB28060 inhibits human c-MET phosphorylation and c-MET-mediated signaling in cancer cells. INCB28060 inhibits c-MET-dependent cell proliferation and survival, and prevents anchorage-independent cancer cell growth and cell migration.
In vivo
INCB28060 shows strong antitumor activity in c-MET-dependent mouse tumor models, even oral treatment of 0.03 mg/kg INCB28060 causes approximately 50% inhibition of c-MET-phosphorylation. Dose-dependent inhibition of tumor growth is observed in tumor-bearing mice.
Features
INCB28060 is inactive against RONβ, another member of the c-MET RTK family, as well as EGFR and HER-3, members of the EGFR RTK family.
