CH5424802

立即咨询

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。

CAS NO:

1256580-46-7

包装与价格：

包装	价格(元)
5mg	电议
50mg	电议

产品介绍

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 SMILES	CCC1=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 tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation 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.