ad80

Description: AD80 is a novel multikinase inhibitor that shows strong activity against human RET, BRAF, S6K, and SRC but were much less active than either AD57 or AD58 against mTOR. AD57 was identified using a Ret-kinase-driven Drosophila model of multiple endocrine neoplasia type 2 and kinome-wide drug profiling, AD57 rescues oncogenic Ret-induced lethality, whereas related Ret inhibitors imparted reduced efficacy and enhanced toxicity. The IC50 value for RET is 4 nM. On the basis of in vitro human kinase profiles, AD80 and AD81 inhibit RET, RAF, SRC and S6K, with greatly reduced mTOR activity relative to AD57 and AD58. AD80 inhibits proliferation of MZ-CRC-1 and TT thyroid cancer cells in culture, probably through the induction of apoptosis.

References: Nature. 2012 Jun 6; 486(7401):80-4