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CCT128930
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。
CCT128930图片
CAS NO:885499-61-6
规格:98%
分子量:341.84
包装与价格:
包装价格(元)
50mg电议
100mg电议

产品介绍
AKT inhibitor
CAS:885499-61-6
分子式:C18H20ClN5
分子量:341.84
纯度:98%
存储:Store at -20°C

Background:

CCT128930 is a potent, selective, novel and ATP-competitive inhibitor for AKT2 (IC50= 6 nM). It also has 28-fold and 20-fold selectivity over PKA kinase (IC50= 168 nM) and p70S6K (IC50= 120 nM), respectively.


Akt (protein kinase B) is a serine/threonine-specific protein kinase that plays a key role in multiple cellular processes such as glucose metabolism, apoptosis, cell proliferation, transcription and cell migration.


In multi tumor cell line, CCT128930 showed antiproliferative effect and blocked the phosphorylation of various Akt substrates. In PTEN-null human glioblastoma cells (U87MG), CCT128930 treatment led to a G1 arrest associated with Akt pathway suppression. [1]


In U87MG tumor xenografts, CCT128930 inhibited the phosphorylation of Akt downstream biomarkers. In U87MG, HER-2 positive and IK3CA-mutant BT474 human breast cancer xenografts, antitumor activity were recorded as tumor volume decreased. CCT128930-treated mouse whisker folliciles in vivo and human hair follicles treated ex vivo exerted prominent reduction in pThr246 PRAS40. [1]


Reference:
1. Yap TA, Walton MI, Hunter LJ 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.