Selpercatinib HCl (LOXO-292; ARRY-192; Retevmo), the hydrochloride salt of Selpercatinib, is an orally bioavailable and highly selective RET (REarranged during Transfection) tyrosin kinase inhibitor approved for cancer treatment. It inhibits RET 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 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.
纯度:≥98%
CAS:2306313-13-1