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CH5424802
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
CH5424802图片
CAS NO:1256580-46-7
包装与价格：
包装价格(元)
5mg询价
50mg询价

CH5424802 (CH5424802) 是一种有效的、选择性的、可口服的 ALK 抑制剂，IC50 为 1.9 nM，Kd 值为 2.4 nM（以 ATP 竞争方式），还抑制 ALK F1174L 和 ALK R1275Q，IC50 为 1 nM和 3.5 nM，分别。 CH5424802 展示了有效的中枢神经系统 (CNS) 渗透。
Cas No.1256580-46-7
别名艾乐替尼; CH5424802; RO5424802; AF802
化学名9-ethyl-6,6-dimethyl-8-(4-morpholin-4-ylpiperidin-1-yl)-11-oxo-5H-benzo[b]carbazole-3-carbonitrile
Canonical SMILESCCC1=C(C=C2C(=C1)C(=O)C3=C(C2(C)C)NC4=C3C=CC(=C4)C#N)N5CCC(CC5)N6CCOCC6
分子式C30H34N4O2
分子量482.62
溶解度≥ 4.83mg/mL in DMSO with ultrasonic and warming
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

CH5424802 is a potent and selective ALK inhibitor.

Anaplastic lymphoma kinase (ALK) is a tyrosine kinase that is constitutively activated in certain cancers. .

In vitro: In cell free assays the IC50 of CH5424802 for enzyme activity of ALK was 1.9 nM; the dissociation constant (KD) value for ALK in an ATP-competitive manner was 2.4 nM. The inhibitory activity for two hot spot-activating mutations (F1174L and R1275Q) in neuroblastoma was comparable to that for wildtype ALK [1].

In vivo: In the NCI-H2228 model, oral administration of CH5424802 resulted in dose-dependent tumor growth inhibition (ED50 = 0.46 mg/kg) and tumor regression. Moreover, treatment of 20 mg/kg CH5424802 showed rapid tumor regression and tumor regrowth did not occur throughout the 4-week drug-free period [2].

Clinical trial: No clinical data are available currently.

Reference:
[1] Sakamoto H, Tsukaguchi T, Hiroshima S, Kodama T, Kobayashi T, Fukami TA, Oikawa N, Tsukuda T, Ishii N, Aoki Y.  CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011 May 17;19(5):679-90.

 
 
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