PF06463922

CAS NO. 1454846-35-5
英文品名 PF-06463922
中文品名 PF-06463922
分子式 C21H19FN6O2
分子量 406.15
规格/纯度 98%
供应能力 can supply g scale
别名 PF 06463922;PF06463922
产品简述 PF-06463922 is a novel, orally available, CNS-ation. Furthermore, PF-06463922 demonstrated antitumorpenetrant, ATP-competitive inhibitor of ALK/ROS1 with Ki of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively.
详细说明 PF-06463922 demonstrates significant cell activity against ALK and a large set of ALK clinical mutations with IC50 ranging from 0.2 nM-77 nM. PF-06463922 exhibited subnanomolar cellular potency against oncogenic ROS1 fusions and inhibited the crizotinib-refractory ROS1(G2032R) mutation and the ROS1(G2026M) gatekeeper mutation. Compared with crizotinib and the second-generation ALK/ROS1 inhibitors ceritinib and alectinib, PF-06463922 showed significantly improved inhibitory activity against ROS1 kinase. in vivo: PF-06463922 showed marked antitumor activity in tumor models expressing FIG-ROS1, CD74-ROS1, and the CD74-ROS1(G2032R) mutation. Furthermore, PF-06463922 demonstrated antitumor activity in a genetically engineered mouse model of FIG-ROS1 glioblastoma.