856692-39-2
中文名称
化合物 CEP-14083
英文名称
Urea, N'-(4,5,6,11,12,13-hexahydro-2-Methyl-4-oxo-11-propyl-2H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-8-yl)-N-Methyl-N-phenyl-
CAS
856692-39-2
分子式
C31H30N6O2
分子量
518.609
MOL 文件
856692-39-2.mol
856692-39-2 结构式
基本信息
中文别名
化合物 CEP-14083 英文别名
CEP-14083DRYABXKGCXCACQ-UHFFFAOYSA-N
Urea, N'-(4,5,6,11,12,13-hexahydro-2-Methyl-4-oxo-11-propyl-2H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-8-yl)-N-Methyl-N-phenyl-
应用领域
用途一
CEP-14083 is a potent ALK inhibitor that has shown activity in an NPM/ALK?–carrying T-cell lymphoma in vitro study. Presumably, this compound binds to the hinge region of the kinase in an ATP-competitive manner. CEP-14083 displays a potent activity against ALK in enzymatic assays (IC50 = 11 nmol/L). Further, CEP-14083 is also able to inhibit the insulin receptor at a concentration within a nanomolar range. In a preclinical assay, CEP-14083 showed that, via NPM/ALK TK inhibition, it could control the expression of molecules that determine T-cell identity and signaling in lymphoma cells. CEP-14083 has shown preclinical activity in both cell lines and animal models harboring ALK alteration.