| 货号 | 5640/50 |
| 别名 | (10R)-7-Amino-12-fluoro-10,15,16,17 |
| 供应商 | Tocris |
| 生物活性 | High affinity and selective ALK and ROS1 inhibitor (Kivalues 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. |
| 运输条件 | Blue Ice |
| 存放说明 | -20℃ |
| 纯度 | >98 % |
| 计算分子量 | 406.41 |
| 分子式 | C21H19FN6O2< |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO and to 100 mM in ethanol |
| 参考文献 | Zouet al (2015) PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations. Proc.Natl.Acad.Sci.U.S.A. 112 3493. PMID: 25733882. Johnsonet al (2014) 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. J.Med.Chem. 57 4720. PMID: 24819116. |