GDC-0349 (RG7603)

Description: GDC-0349(also known as RG-7603) is a novel, potent, orally bioavailable and selective ATP-competitive inhibitor of mTOR (mammalian target of rapamycin) with potential antitumor activity. It inhibits mTOR with a Ki of 3.8 nM, and exhibits 790-fold higher selectivity over PI3Kalpha and other 266 kinases. GDC-0349 showed potent antiproliferative activity in vitro and high antitumor efficacy in vivo. GDC-0349 inhibited tumor growth dose-dependently in athymic mice in a MCF7-neo/Her2 tumor xenograft model. GDC-0349 was developed by GeneTech for treatment of locally advanced or metastatic solid tumors or non Hodgkin's lymphoma.

References:J Med Chem. 2013 Apr 11; 56(7):3090-101; ACS Med Chem Lett. 2012 Nov 29; 4(1):103-7.