Structure of the Human Anaplastic Lymphoma Kinase in Complex with PF- 06463922 ((10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16, 17-tetrahydro-2H-8,4-(metheno)pyrazolo(4,3-h)(2,5,11) benzoxadiazacyclotetradecine-3-carbonitrile).

Structure of the Human Anaplastic Lymphoma Kinase in Complex with PF- 06463922 ((10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16, 17-tetrahydro-2H-8,4-(metheno)pyrazolo(4,3-h)(2,5,11) benzoxadiazacyclotetradecine-3-carbonitrile). Descriptor: (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile, ALK TYROSINE KINASE RECEPTOR Authors: McTigue, M.A, Deng, Y.L, Liu, W, Brooun, A, Stewart, A.E. Deposit date: 2014-01-14 Release date: 2014-05-28 Last modified: 2023-12-20 Method: X-RAY DIFFRACTION (2.05 Å) Cite: Discovery of (10R)-7-Amino-12-Fluoro-2,10,16-Trimethyl-15-Oxo-10,15,16,17-Tetrahydro-2H-8,4-(Metheno)Pyrazolo[4,3-H][2,5,11]Benzoxadiazacyclotetradecine-3-Carbonitrile (Pf-06463922), a Macrocyclic Inhibitor of Alk/Ros1 with Pre-Clinical Brain Exposure and Broad Spectrum Potency Against Alk-Resistant Mutations. J.Med.Chem., 57, 2014

与PF-06463922结合的人间变性淋巴瘤激酶（Anaplastic Lymphoma Kinase, ALK）的晶体结构，其中PF-06463922的化学全称为(10R)-7-氨基-12-氟-2,10,16-三甲基-15-氧代-10,15,16,17-四氢-2H-8,4-(亚甲基)吡唑并[4,3-h][2,5,11]苯并氧二氮杂环十四烷-3-甲腈。描述项：(10R)-7-氨基-12-氟-2,10,16-三甲基-15-氧代-10,15,16,17-四氢-2H-8,4-(亚甲基)吡唑并[4,3-h][2,5,11]苯并氧二氮杂环十四烷-3-甲腈，ALK酪氨酸激酶受体（ALK TYROSINE KINASE RECEPTOR）。作者：McTigue, M.A.、Deng, Y.L.、Liu, W.、Brooun, A.、Stewart, A.E.。提交日期：2014-01-14。发布日期：2014-05-28。最后修改日期：2023-12-20。实验方法：X射线衍射（X-RAY DIFFRACTION），分辨率为2.05埃（Å）。引用文献：《(10R)-7-氨基-12-氟-2,10,16-三甲基-15-氧代-10,15,16,17-四氢-2H-8,4-(亚甲基)吡唑并[4,3-h][2,5,11]苯并氧二氮杂环十四烷-3-甲腈（PF-06463922）：一种兼具临床前脑暴露活性与抗ALK耐药突变广谱强效性的ALK/ROS1大环类抑制剂》，刊载于《药物化学杂志》（J. Med. Chem.）2014年第57卷。