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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-Akt-CCT128930
CCT128930

Chemical Structure : CCT128930

CAS No.: 885499-61-6

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CCT128930 (CCT 128930;CCT-128930)

货号: PC-43440Not For Human Use, Lab Use Only.

CCT128930 is a potent, selective, ATP-competitive AKT inhibitor with IC50 of 6 nM (AKT2), 28-fold selectivity over the closely related PKA.

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5 mg ￥1180 In stock
10 mg ￥1880 In stock
25 mg ￥3280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CCT128930 is a potent, selective, ATP-competitive AKT inhibitor with IC50 of 6 nM (AKT2), 28-fold selectivity over the closely related PKA.
CCT128930 also exhibits 20-fold selectivity over p70S6K (IC50=120 nM).
CCT128930 shows growth inhibition for U87MG human glioblastoma cells (IC50=6.3 uM), for LNCaP human prostate cancer cells (IC50=0.35 uM), and for PC3 human prostate cancer cells (IC50=1.9 uM) consistent with AKT pathway blockade.
CCT128930 blocks the phosphorylation of several downstream AKT biomarkers in U87MG tumor xenografts, indicating AKT inhibition in vivo.
CCT128930 demonstrates antitumor activity in U87MG and HER2-positive, PIK3CA-mutant BT474 human breast cancer xenografts.

物理化学性质&存储条件

分子量 341.84
分子式 C18H20ClN5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

4-Piperidinamine, 4-[(4-chlorophenyl)methyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-

参考文献

1. Caldwell JJ, et al. J Med Chem. 2008 Apr 10;51(7):2147-57.

2. Yap TA, et al. Mol Cancer Ther. 2011 Feb;10(2):360-71.

3. Yap TA, et al. Clin Cancer Res. 2012 Jul 15;18(14):3912-23.

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