loxo-292-arry-192

Description: Ret-IN-1, a Selpercatinib analog, is a novel, potent, orally bioavailable and selective a RET kinase inhibitor with anticancer activity. It is an investigational drug in clinical development for the treatment of patients with cancers that harbor abnormalities in the rearranged during transfection (RET) kinase. Selpercatinib (LOXO-292; ARRY-192; Retevmo) is a potent, orally bioavailable and highly selective RET (REarranged during Transfection) tyrosin kinase inhibitor with IC50 of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M), and RET (G810R), respectively. As of May 2020, Selpercatinib was approved by the US FDA for the treatment of lung and thyroid cancers. LOXO-292 selectively binds to and targets various RET mutants and RET-containing fusion products, which leads to an inhibition of cell growth of tumors cells that exhibit increased RET activity.

References: WO2018071447A1.

Related CAS #: 2152628-33-4 (free base) 2306313-16-4 (tosylate) 2306313-17-5 (mesylate) 2306313-13-1 (HCl) 2306313-14-2 (sulfate) 2306313-19-7 (besylate) 2306313-23-3 (maleate) 2306313-28-8 (fumarate) 2306313-27-7 (tartrate) 2306313-29-9 (citrate)