In addition to our lead kinase inhibitor MGCD265, MethylGene has also developed MG516, a novel multi-targeted kinase inhibitor that has demonstrated potent inhibition of enzymatic activities in vitro and in multiple cell-based assays and has shown up to 100% of tumor growth inhibition against a number of tumor types in xenograft studies. The profile of MG516 features the inhibition of a novel spectrum of targets which include members of the Eph receptor family, the Met receptor, the Ret receptor tyrosine kinase, and all three vascular endothelial growth factor receptors (VEGFR 1, 2, 3). The inclusion of Eph and Ret as targets, in addition to Met, is important due to their overexpression and/or mutation in a number of cancers. Eph is overexpressed in several cancers including gastric, lung, breast, ovarian, uterine, prostate, esophageal, brain and skin while the activating mutations of Ret are primarily associated with medullary thyroid carcinoma (MTC).
MG516 is in advanced preclinical development and ready to commence IND-enabling studies.
Posters & Publications
|Beaulieu, N. et al., AACR 2013 Annual Meeting, April 2013Preclinical characterization of MG516, a novel inhibitor of receptor tyrosine kinases involved in resistance to targeted therapies|
|Raeppel S, et al, 2010 Bioorg Med Chem Lett. 20(9):2745-9.Identification of a novel series of potent RON receptor tyrosine kinase inhibitors.|
|Maroun, C. et al. AACR 100th Annual Meeting, April 2009Preclinical development of a novel oral multi-targeted kinase inhibitor with potent in vivo antitumor activity (MG516)|