PF06463922原料

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-penetrant, 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.

湖北帝柏化工有限公司总部成立于09年，位于湖北省长江中游两岸，中国历史文化名城之一的“荆州”。帝柏化工先后创立荆州区精细化工原料厂、孝感云梦医药原料厂两大生产型单位。是省重点扶持集研发、生产、销售一体的高新技术产业单位，被誉为湖北化工行业“企业之星”。