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[Stock]: less than 500g
[Customer Synthesis]: Avilable
Biological Activity of Lorlatinib(PF-06463922,1454846-35-5)
Description High affinity and selective ALK and ROS1 inhibitor (Ki values are <0.02, <0.07 and 0.7 nM for ROS1, wild-type ALK and ALK-L1196M, respectively). Exhibits >100-fold selectivity for ROS1 over a panel of 204 other kinases. Inhibits proliferation of BaF3 cells containing crizotinib-resistant ROS1 mutation in vitro. Inhibits tumor growth in relevant mouse models. Orally available and brain penetrant.
PF-06463922 Usage And Synthesis
|Uses||Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase that promotes cell proliferation and blocks apoptosis. PF-06463922 is an ATP-competitive, selective inhibitor of ALK (Ki = < 0.07 nM) and c-Ros oncogene 1 (ROS1, Ki = 0.7 nM). It has strong activity against all known ALK and ROS1 mutants identified in patients, including the EML4-L1196M mutant of ALK (Ki = < 0.02 nM). PF-06463922 is orally available, displaying inhibition of ALK phosphorylation and antitumor efficacy in a xenograft model expressing EML4-L1196M ALK. It demonstrates efficient blood-brain barrier penetration, produces brain tumor regression in mice harboring EML4-ALK tumors, and increases overall survival.[Cayman Chemical]|
|Enzyme inhibitor||This potent, dual ALK/ROS1 inhibitor (FW = 406.41 g/mol; CAS 1454846- 35-5), also named (10R)-7-amino-12-fluoro-10,15,16,17-tetrahydro- 2,10,16-trimethyl-15-oxo-2H-4,8-methenopyrazolo[4,3- h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile, targets the protooncogene tyrosine-protein kinase ROS1 (Ki < 0.02 nM) as well as wild-type anaplastic lymphoma kinase ALKWT (Ki < 0.07 nM) and its Leu-to-Met mutant ALKL1196M (Ki of = 0.7 nM). PF-06463922 significantly inhibits cell proliferation and induces cell apoptosis in the HCC78 human NSCLC cells harboring SLC34A2-ROS1 fusions and the BaF3-CD74-ROS1 cells expressing human CD74-ROS1|
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