CCT128930 HCl

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Chemical Structure| 2453324-32-6 同义名 : CCT128930 hydrochloride
CAS号 : 2453324-32-6
货号 : A1221053
分子式 : C18H21Cl2N5
纯度 : 99%+
分子量 : 378.3
MDL号 : MFCD32667039
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 18 mg/mL(47.58 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 CCT128930 hydrochloride is a potent and selective AKT inhibitor, with an IC50 of 6 nM. It exhibits 28-fold selectivity against the closely related PKA kinase, with an IC50 of 168 nM, and 20-fold selectivity over p70S6K, with an IC50 of 120 nM. This selectivity is achieved through targeting Met282 of AKT (Met173 of PKA-AKT chimera). CCT128930 hydrochloride induces cell cycle arrest, DNA damage, and autophagy, demonstrating significant antitumor activity[1][2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.64mL

0.53mL

0.26mL

13.22mL

2.64mL

1.32mL

26.43mL

5.29mL

2.64mL
参考文献

[1]Yap TA et al. Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930. Mol Cancer Ther. 2011 Feb;10(2):360-71.

[2]Wang FZ, et al. CCT128930 induces cell cycle arrest, DNA damage, and autophagy independent of Akt inhibition. Biochimie. 2014;103:118-125.