Sitravatinib (MGCD516)

Information Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multipleRTKsinvolved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl. Targets DDR2 (Cell-free assay); EPHA3 (Cell-free assay); Axl (Cell-free assay); Mer (Cell-free assay); VEGFR3 (FLT4) (Cell-free assay) 27977,0.5 nM; 1 nM; 1.5 nM; 2 nM; 2 nM In vitro MGCD516 (Sitravatinib), is an oral, potent small molecule inhibitor of a closely related spectrum of RTKs including RET, the split RTKs (VEGFR, PDGFR and KIT), TRK family, DDR2, MET and AXL. MGCD516 treatment resulted in significant blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro. In vivo Sitravatinib has demonstrated antitumor activity in nonclinical cancer models harboring genetic alterations of sitravatinib targets, including rearrangement of RET, NTRK, or CHR4q12 amplification. MGCD516 treatment of tumor xenografts in vivo resulted in significant suppression of tumor growth. Efficacy of MGCD516 was superior to imatinib and crizotinib, two other well-studied multi-kinase inhibitors with overlapping target specificities, both in vitro and in vivo. Cell Research(from reference) Cell lines：DDLS, LS141 and MPNST Concentrations：62.5, 125, 250, 500, 1000, 2000 nM/L Incubation Time：72 h

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