Pricing updated 2019-04-25. Prices are subject to change without notice.
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).1 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).1,2,3 PF-06463922 is orally available, displaying inhibition of ALK phosphorylation and antitumor efficacy in a xenograft model expressing EML4-L1196M ALK.1,4 It demonstrates efficient blood-brain barrier penetration, produces brain tumor regression in mice harboring EML4-ALK tumors, and increases overall survival.2
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Johnson, T.W., Richardson, P.F., Bailey, S., et al. Discovery of (10R)-
Awad, M.M., and Shaw, A.T. ALK inhibitors in non-
Zou, H.Y., Li, Q., Engstrom, L.D., et al. PF-
Yamazaki, S., Lam, J.L., Zou, H.Y., et al. Translational pharmacokinetic-