Lorlatinib (Standard)

Lorlatinib (Standard) is the analytical standard of Lorlatinib. This product is intended for research and analytical applications. Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has K_is of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK^L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC₅₀s of 15-43 nM (ALK^L1196), 14-80 nM (ALK^G1269A), 38-50 nM (ALK^1151Tins), 77-113 nM (ALK^G1202R), respectively^[1][2][3]. IC50 & Target:IC50: 15-43 nM (ALK^L1196), 14-80 nM (ALK^G1269A), 38-50 nM (ALK^1151Tins), 77-113 nM (ALK^G1202R)^[3]
Ki: <0.07 nM (ALK^WT), 0.6 nM (ALK^L1996M), 0.9 nM (ALK^G1269A), 0.1 nM (ALK^1151Tins), <0.1 nM (ALK^L1152R), 0.2 nM (ALK^S1206Y), <0.1 nM (ALK^C1156Y), <0.1nM (ALK^F1174L)^[3]