Savolitinib

Savolitinib is an inhibitor of c-Met (IC50 = 5 nM). It is selective for c-Met over a panel of 274 other kinases at 1 µM. Savolitinib inhibits c-Met autophosphorylation in NCI H441 human non-small cell lung cancer (NSCLC) cells (IC50 = 3 nM). It also inhibits proliferation of NCI H441 cells induced by HGF (Cay-32052, IC50 = 6 nM) and in a panel of gastric cancer cells with dysregulated c-Met (EC50s = 0.6-14.7 nM). Savolitinib (3 mg/kg) inhibits intratumor c-Met autophosphorylation by 94% and reduces tumor growth in an Hs 746T human stomach cancer mouse xenograft model.Formal Name: 1-[(1S)-1-imidazo[1,2-a]pyridin-6-ylethyl]-6-(1-methyl-1H-pyrazol-4-yl)-1H-1,2,3-triazolo[4,5-b]pyrazine. CAS Number: 1313725-88-0. Synonyms: AZD6094, HMPL-504, Volitinib. Molecular Formula: C17H15N9. Formula Weight: 345.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 1 mg/ml, DMSO:PBS (pH 7.2) (1:20): 0.05 mg/ml. lambdamax: 225, 348 nm. SMILES: C[C@@H](C1=CN2C(C=C1)=NC=C2)N3C4=NC(C5=CN(C)N=C5)=CN=C4N=N3. InChi Code: InChI=1S/C17H15N9/c1-11(12-3-4-15-18-5-6-25(15)10-12)26-17-16(22-23-26)19-8-14(21-17)13-7-20-24(2)9-13/h3-11H,1-2H3/t11-/m0/s1. InChi Key: XYDNMOZJKOGZLS-NSHDSACASA-N.