INCB28060


CAS No. : 1029712-80-8

INCB28060,1029712-80-8
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000180
Synonyms:2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide
Molecular Formula:C23H17FN6O
Molecular Weight:412.4
Target:c-MET
IC50:0.13±0.05 nM( for recombinant human wild-type c-MET) [1]
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Appearance:Yellow solid powder
Purity: > 98%
Cat No:I000180
Cas No:1029712-80-8
Product-Name:INCB28060
InChIKey:LIOLIMKSCNQPLV-UHFFFAOYSA-N

Description:
IC50 Value: 0.13±0.05 nM( for recombinant human wild-type c-MET) [1]
INCB28060 is a novel orally active inhibitor (IC50: 0.13nM) of c-MET kinase. INCB28060 potently and specifically inhibits c-MET enzyme activity, c-MET-mediated signal transduction, and the c-MET-dependent neoplastic phenotype of tumor cells .
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. This inhibitor potently blocks c-MET phosphorylation and activation of its key downstream effectors in c-MET-dependent tumor cell lines [1].
in vivo: 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, and the inhibitor is well tolerated at doses that achieve complete tumor inhibition [1]. Activated c-MET positively regulates the activity of epidermal growth factor receptors (EGFR) and HER-3, as well as expression of their ligands. These effects are reversed with INCB28060 treatment.
Toxicity: INCB28060 was well tolerated at all doses during the treatment periods, with no evidence of overt toxicity or weight loss [1].
Clinical trial: INC-280 and Erlotinib Hydrochloride in Treating Patients With Non-small Cell Lung Cancer. Phase 1

1:Clin Cancer Res. 2011 Nov 15;17(22):7127-38. doi: 10.1158/1078-0432.CCR-11-1157. Epub 2011 Sep 14. A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3.Liu X,Wang Q,Yang G,Marando C,Koblish HK,Hall LM,Fridman JS,Behshad E,Wynn R,Li Y,Boer J,Diamond S,He C,Xu M,Zhuo J,Yao W,Newton RC,Scherle PA, PMID: 21918175 DOI: 10.1158/1078-0432.CCR-11-1157
Abstract: PURPOSE: The c-MET receptor tyrosine kinase plays important roles in the formation, progression, and dissemination of human cancer and presents an attractive therapeutic target. This study describes the preclinical characterization of INCB28060, a novel inhibitor of c-MET kinase.EXPERIMENTAL DESIGN: Studies were conducted using a series of in vitro and in vivo biochemical and biological experiments.RESULTS: 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. This inhibitor potently blocks c-MET phosphorylation and activation of its key downstream effectors in c-MET-dependent tumor cell lines. As a result, INCB28060 potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis in vitro. 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, and the inhibitor is well tolerated at doses that achieve complete tumor inhibition. In a further exploration of potential interactions between c-MET and other signaling pathways, we found that activated c-MET positively regulates the activity of epidermal growth factor receptors (EGFR) and HER-3, as well as expression of their ligands. These effects are reversed with INCB28060 treatment. Finally, we confirmed that circulating hepatocyte growth factor levels are significantly elevated in patients with various cancers.CONCLUSIONS: Activated c-MET has pleiotropic effects on multiple cancer-promoting signaling pathways and may play a critical role in driving tumor cell growth and survival. INCB28060 is a potent and selective c-MET kinase inhibitor that may have therapeutic potential in cancer treatment.
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