| 货号 | 18371-1mg |
| 描述 | 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 |
| 别名 | Lorlatinib; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Johnson, T.W.,Richardson, P.F.,Bailey, S., et al. 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 anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations. Journal of Medicinal Chemistry 57(11), 4720-4744 (2014). 2.Awad, M.M. and Shaw, A.T. ALK inhibitors in non-small cell lung cancer: Crizotinib and beyond. Clin. Adv. Hematol. Oncol. 12(7), 429-439 (2014). 3.Zou, H.Y.,Li, Q.,Engstrom, L.D., et al. PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations. Proceedings of the National Academy of Sciences of the United States of America 112(11), 3493-3498 (2015). 4.Yamazaki, S.,Lam, J.L.,Zou, H.Y., et al. Translational pharmacokinetic-pharmacodynamic modeling for an orally available novel inhibitor of anaplastic lymphoma kinase and c-Ros oncogene 1. Journal of Pharmacology and Experimental Therapeutics 351, 67-76 (2014). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 406.4 |
| 分子式 | C21H19FN6O2 |
| CAS号 | 1454846-35-5 |
| 稳定性 | ≥ 2 years |
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