PF-06463922

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 = i = 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.Formal Name: (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. CAS Number: 1454846-35-5. Synonyms: Lorlatinib. Molecular Formula: C21H19FN6O2. Formula Weight: 406.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/mL, DMSO: 5 mg/mL, Ethanol: 1 mg/mL, Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/mL. lambdamax: 319 nm. SMILES: FC1=CC=C(C(N(C)CC2=NN(C)C(C#N)=C32)=O)C([C@@H](C)OC4=C(N)N=CC3=C4)=C1. InChi Code: InChI=1S/C21H19FN6O2/c1-11-15-7-13(22)4-5-14(15)21(29)27(2)10-16-19(17(8-23)28(3)26-16)12-6-18(30-11)20(24)25-9-12/h4-7,9,11H,10H2,1-3H3,(H2,24,25)/t11-/m1/s1. InChi Key: IIXWYSCJSQVBQM-LLVKDONJSA-N.