CH5424802

An orally available inhibitor of ALK

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库存: 现货

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5mg

￥762.00

610.00

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50mg

￥2112.00

1690.00

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货号: ajci16292
CAS: 1256580-46-7
别名: 艾乐替尼; CH5424802; RO5424802; AF802
分子式: C30H34N4O2
分子量: 482.62
纯度: >98%
溶解度: ≥ 4.83mg/mL in DMSO with ultrasonic and warming
储存: Store at -20°C
库存: 现货

Background

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.