A potent c-Met inhibitor (IC50 = 0.42 nM); >2

Glumetinib – 5 mg

Brand:
Cayman
CAS:
1642581-63-2
Storage:
-20
UN-No:
Non-Hazardous - /

Glumetinib is a potent inhibitor of c-Met (IC50 = 0.42 nM).{52121} It is greater than 2,400-fold selective for c-Met over a panel of 312 kinases. Glumetinib (0.001-1 μM) inhibits c-Met phosphorylation in and proliferation of MET-overexpressing EBC-1 lung and MKN45 gastric cancer cells. It inhibits NCI H441 cell motility and invasion induced by hepatocyte growth factor (HGF) when used at a concentration of 10 nM. Glumetinib (2.5-10 mg/kg) reduces tumor volume in MKN45, SNU-5, and EBC-1 mouse xenograft models. It also reduces tumor growth in MET amplification-containing non-small cell lung cancer (NSCLC) and hepatocellular carcinoma (HCC) patient-derived xenograft (PDX) mouse models.  

 

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SKU: 28952 - 5 mg Category:

Description

A potent c-Met inhibitor (IC50 = 0.42 nM); >2,400-fold selective for c-Met over a panel of 312 kinases; inhibits c-Met phosphorylation in and proliferation of MET-overexpressing EBC-1 lung and MKN45 gastric cancer cells from 0.001-1 μM; inhibits HGF-induced NCI H441 cell motility and invasion at 10 nM; reduces tumor volume in MKN45, SNU-5, and EBC-1 mouse xenograft models from 2.5-10 mg/kg; reduces tumor growth in MET amplification-containing NSCLC and HCC PDX mouse models

Formal name: 6-(1-methyl-1H-pyrazol-4-yl)-1-[[6-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl]sulfonyl]-1H-pyrazolo[4,3-b]pyridine

Synonyms:  SCC244

Molecular weight: 459.5

CAS: 1642581-63-2

Purity: ≥98%

Formulation: A crystalline solid

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