SAR125844

SAR125844 is an inhibitor of the receptor tyrosine kinase c-Met (IC50 = 4 nM). It is selective for c-Met over tropomyosin-related kinase A (TrkA), TrkB, PDGFRalpha, Axl, and Mer (IC50s = 39, 280, 55, 87, and 105 nM, respectively). SAR125844 inhibits the proliferation of MKN45 gastric cancer cells (IC50 = 7 nM). In vivo, SAR125844 (20 mg/kg) inhibits intratumoral c-Met phosphorylation in a MET-amplified Hs 746T gastric cancer mouse xenograft model. SAR125844 (10-45 mg/kg) also reduces tumor volume in Hs 746T and SNU-5 gastric cancer mouse xenograft models.Formal Name: N-[6-[[6-(4-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]thio]-2-benzothiazolyl]-N'-[2-(4-morpholinyl)ethyl]-urea. CAS Number: 1116743-46-4. Molecular Formula: C25H23FN8O2S2. Formula Weight: 550.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: Slightly Soluble, DMSO: Slightly Soluble. lambdamax: 228, 282 nm. SMILES: O=C(NCCN1CCOCC1)NC2=NC3=CC=C(C=C3S2)SC4=NN=C5C=CC(C6=CC=C(F)C=C6)=NN45. InChi Code: InChI=1S/C25H23FN8O2S2/c26-17-3-1-16(2-4-17)19-7-8-22-30-31-25(34(22)32-19)37-18-5-6-20-21(15-18)38-24(28-20)29-23(35)27-9-10-33-11-13-36-14-12-33/h1-8,15H,9-14H2,(H2,27,28,29,35). InChi Key: ODIUNTQOXRXOIV-UHFFFAOYSA-N.