Sitravatinib (MGCD516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.
Description :
A novel, broad spectrum small molecule inhibitor that blocks a wide array of RTKs known to be amplified/overexpressed in sarcomas, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl (IC50=1.5-30 nM); significantly blocks the phosphorylation of potential driver RTKs and induces potent anti-proliferative effects in vitro; suppresses tumor growth in tumor xenografts in vivo.
Lung Cancer
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[1]. MGCD516 treatment resulted in significant blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro[2].
Sitravatinib has demonstrated antitumor activity in nonclinical cancer models harboring genetic alterations of sitravatinib targets, including rearrangement of RET, NTRK, or CHR4q12 amplification[1]. 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[2].