规格

价格

库存

数量

1 mg

¥ 439

现货

2 mg

¥ 579

现货

5 mg

¥ 790

现货

10 mg

¥ 1,290

现货

25 mg

¥ 2,180

现货

50 mg

¥ 3,250

现货

100 mg

¥ 4,650

现货

1 mL x 10 mM (in DMSO)

¥ 979

现货

生物活性

产品描述	CCT128930 hydrochloride (CCT128930 hydrochloride) is a potent and selective inhibitor of AKT with IC50 of 6 nM. CCT128930 hydrochloride induces cell cycle arrest, DNA damage, and autophagy. CCT128930 hydrochloride has 28-fold selectivity over the closely related PKA kinase (IC50: 168 nM) through the targeting of Met282 of AKT, as well as 20-fold selectivity over p70S6K (IC50: 120 nM).
靶点活性	PKA:168 nM, p70 S6K:120 nM, Akt2:6 nM
体外活性	In U87MG human glioblastoma cells, CCT128930 hydrochloride(0.1-60 μM; 1 hour) shows an initial induction of AKT phosphorylation at serine 473 up to 20 μM, followed by a decreased in phosphorylation at higher concentrations[1]. CCT128930 (18.9 μM) hydrochloride causes an increase in phosphorylation of pSer473 AKT after 30 minutes, which is sustained for 48 hours. Total AKT protein signal decreases gradually from 8 hours to 48 hours of treatment[1]. The GI50 values of CCT128930 hydrochloride for growth inhibition are 6.3 μM for U87MG human glioblastoma cells, 0.35 μM for LNCaP human prostate cancer cells, and 1.9 μM for PC3 human prostate cancer cells, all of which are PTEN-deficient human tumor cell lines[1]. CCT128930 hydrochloride inhibits direct substrates of AKT (Ser9 GSK3β, pThr246 PRAS40 and pT24 FOXO1/p32 FOXO3a) at ≥5 μM, and the downstream target, pSer235/236 S6RP at ≥10 μM, with generally constant levels of the respective total proteins and GAPDH[1].
体内活性	CCT128930 hydrochloride shows antitumor activities in U87MG and BT474 human breast cancer xenografts[1].
别名	CCT128930 hydrochloride(885499-61-6 Free base)

化学信息

分子量	378.3
分子式	C₁₈H₂₁Cl₂N₅
CAS No.	2453324-32-6
Smiles	Cl.NC1(Cc2ccc(Cl)cc2)CCN(CC1)c1ncnc2[nH]ccc12
密度	no data available

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 55 mg/mL (145.39 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.29 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6434 mL	13.2170 mL	26.4340 mL	132.1702 mL
5 mM	0.5287 mL	2.6434 mL	5.2868 mL	26.4340 mL
10 mM	0.2643 mL	1.3217 mL	2.6434 mL	13.2170 mL
20 mM	0.1322 mL	0.6609 mL	1.3217 mL	6.6085 mL
50 mM	0.0529 mL	0.2643 mL	0.5287 mL	2.6434 mL
100 mM	0.0264 mL	0.1322 mL	0.2643 mL	1.3217 mL