856692-39-2

中文名稱化合物 CEP-14083

英文名稱 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 結(jié)構(gòu)式

基本信息物理化學(xué)性質(zhì) 應(yīng)用領(lǐng)域常見問題列表

基本信息

中文別名

化合物 CEP-14083

英文別名

CEP-14083
DRYABXKGCXCACQ-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-

物理化學(xué)性質(zhì)

沸點(diǎn)833.7±65.0 °C(Predicted)

密度1.40±0.1 g/cm3(Predicted)

酸度系數(shù)(pKa)13.95±0.20(Predicted)

應(yīng)用領(lǐng)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.

常見問題列表

概述

CEP-14083 是一種與 ATP 競爭的 ALK 激酶抑制劑，其在酶學(xué)實(shí)驗(yàn)中的 IC50 值為 2 nM。CEP-14083 還抑制其他激酶，例如胰島素受體 (IR)，血管內(nèi)皮生長因子受體2 (VEGFR2/KDR/Flk-1)，血管生成素-1 受體 (TIE2) 和雙亮氨酸拉鏈激酶 (DLK)。CEP-14083 抑制 CD274 mRNA 的表達(dá)以及在攜帶 NPM/ALK 的 T 細(xì)胞淋巴瘤 (ALK+TCL) 細(xì)胞中的 NPM/ALK 功能。CEP-14083 有望用于淋巴瘤的研究。