Glumetinib

Glumetinib is a potent inhibitor of c-Met (IC50 = 0.42 nM). 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.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. CAS Number: 1642581-63-2. Synonyms: SCC244. Molecular Formula: C21H17N9O2S. Formula Weight: 459.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 50mg/mL, DMF:PBS (pH 7.2) (1:1): 0.5mg/mL, DMSO: 30mg/mL. lambdamax: 264, 316 nm. SMILES: O=S(N1N=CC2=NC=C(C3=CN(C)N=C3)C=C21)(C4=CN=C5N4C=C(C6=CN(C)N=C6)C=C5)=O. InChi Code: InChI=1S/C21H17N9O2S/c1-27-11-16(7-24-27)14-3-4-20-23-10-21(29(20)13-14)33(31,32)30-19-5-15(6-22-18(19)9-26-30)17-8-25-28(2)12-17/h3-13H,1-2H3. InChi Key: RYBLECYFLJXEJX-UHFFFAOYSA-N.