Sitravatinib malate

Description: Sitravatinib malate is an orally bioavailable receptor inhibitor of tyrosine kinase (RTK) (IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively.) , shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment. Target: TAM Receptor. Smiles: [C@H](CC(O)=O)(C(O)=O)O.C(NC1=CC(F)=C(OC2=C3C(C=C(S3)C4=CC=C(CNCCOC)C=N4)=NC=C2)C=C1)(=O)C5(C(NC6=CC=C(F)C=C6)=O)CC5. References: Patwardhan PP et al. Significant blockade of multiple receptor tyrosine kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preclinical models of sarcoma. Oncotarget, 2016 Jan 26,7(4):4093-109.