Lorlatinib acetate

Description

Lorlatinib PF-06463922 acetate is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib acetate has Kis of 0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALKL1196M, respectively. Lorlatinib acetate targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM ALKL1196 , 14-80 nM ALKG1269A , 38-50 nM ALK1151Tins , 77-113 nM ALKG1202R , respectively.