Sitravatinib

Sitravatinib is a multi-kinase inhibitor. It inhibits 35 kinases (IC50s = 0.5-5,550 nM) in a panel of 55 receptor tyrosine kinases (RTKs). Sitravatinib reduces proliferation of A-673, LPS141, MPNST, DDLS, and Saos-2 cancer cells (IC50s = 1,750, 340.1, 705.7, 266, and 1,830 nM, respectively) and decreases phosphorylation of insulin-like growth factor 1 receptor (IGF1-R), PDGFRbeta, and Akt in these same cells when used at concentrations ranging from 62.5 to 4,000 nM. It decreases tumor growth in LPS141 and MPNST mouse xenograft models when administered at a dose of 15 mg/kg per day.Formal Name: N-[3-fluoro-4-[[2-[5-[[(2-methoxyethyl)amino]methyl]-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide. CAS Number: 1123837-84-2. Synonyms: MGCD-516. Molecular Formula: C33H29F2N5O4S. Formula Weight: 629.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5mg/mL, DMSO: 10mg/mL, Ethanol: 5mg/mL, Ethanol:PBS (pH 7.2) (1:2): 0.3mg/mL. lambdamax: 254, 316 nm. SMILES: FC1=CC(NC(C2(CC2)C(NC3=CC=C(F)C=C3)=O)=O)=CC=C1OC4=C5C(C=C(C6=CC=C(CNCCOC)C=N6)S5)=NC=C4. InChi Code: InChI=1S/C33H29F2N5O4S/c1-43-15-14-36-18-20-2-8-25(38-19-20)29-17-26-30(45-29)28(10-13-37-26)44-27-9-7-23(16-24(27)35)40-32(42)33(11-12-33)31(41)39-22-5-3-21(34)4-6-22/h2-10,13,16-17,19,36H,11-12,14-15,18H2,1H3,(H,39,41)(H,40,42). InChi Key: WLAVZAAODLTUSW-UHFFFAOYSA-N.