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CCT128930

CCT128930

产品编号 T6303   CAS 885499-61-6

CCT128930 是一种 ATP 竞争性,选择性 AKT 抑制剂。它通过靶向 AKT 的 Met282 (PKA-AKT 嵌合体的 Met173),对 PKA 激酶具有 28 倍的选择性,对 p70S6K 具有 20 倍的选择性,具有抗肿瘤活性。 在相同实验条件下,摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性,但盐形式 CCT128930 hydrochloride 的水溶性和稳定性通常比游离态更好。

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CCT128930 Chemical Structure
CCT128930, CAS 885499-61-6
规格 价格/CNY 货期 数量
1 mg ¥ 356 5日内发货
2 mg ¥ 528 5日内发货
5 mg ¥ 977 5日内发货
10 mg ¥ 1,580 5日内发货
25 mg ¥ 2,970 5日内发货
50 mg ¥ 4,790 5日内发货
1 mL * 10 mM (in DMSO) ¥ 1,080 5日内发货

CCT128930 的其他形式现货产品:

CCT128930 hydrochloride
其他形式的 CCT128930:
产品目录号及名称: CCT128930 (T6303)
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纯度: 99.18%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM, 28-fold greater selectivity for Akt2 than the closely related PKA kinase.
靶点活性 Akt2:6 nM
体外活性 CCT128930 exhibits marked antiproliferative activity against PTEN-deficient human tumor cell lines including U87 mg human glioblastoma cells, LNCaP human prostate cancer cells and PC3 human prostate cancer cells with GI50 of 6.3 μM, 0.35 μM and 1.9 μM, respectively. Furthermore, CCT128930 causes a G1 arrest in PTEN-null U87 mg human glioblastoma cells and Akt pathway blockade. [1]
体内活性 CCT128930 at 25 mg/kg i.p. shows a marked antitumor effect in established PTEN-null U87 mg human glioblastoma xenografts with a treated:control (T/C) ratio of 48% on day 12. In HER2-positive, PIK3CA-mutant BT474 human breast cancer xenografts, CCT128930 at 40 mg/kg also produces a profound antitumor effect with complete growth arrest and a T/C ratio of 29% on day 22. CCT128930 administrated via i.v. reaches a peak concentration of 6.4 μM in plasma and is eliminated with a relatively short half-life, high volume of distribution, and rapid clearance, giving an area under the curve AUC0-∞ of 4.6 μM h. CCT128930 administrated via i.p. leads to the peak plasma drug concentration of 1.3 μM and the corresponding AUC0-∞ of 1.3 μM·h. Oral CCT128930 administration leads to the peak plasma concentration of only 0.43 μM and a correspondingly low AUC0-∞ of 0.4 μM·h. [1]
激酶实验 Kinase assays: Profiling against 50 different human kinases is carried out using 10 μM CCT128930 at an ATP concentration equivalent to the Km for each enzyme.
细胞实验 Cells are seeded in 96-well plates and allowed to attach for 36 hours to ensure exponential growth prior to treatment. In vitro antiproliferative activity is determined using a 96-hour SRB assay. TCA-fixed cells are stained for 30 minutes with 0.4% (wt/vol) SRB dissolved in 1% acetic acid. At the end of the staining period, SRB is removed and cultures are quickly rinsed four times with 1% acetic acid to remove unbound dye. The acetic acid is poured directly into the culture wells from a beaker. This procedure permits rinsing to be performed quickly so that desorption of protein-bound dye does not occur. Residual wash solution is removed by sharply flicking plates over a sink, which ensures the complete removal of rinsing solution. Because of the strong capillary action in 96-well plates, draining by gravity alone often fails to remove the rinse solution when plates are simply inverted. After being rinsed, the cultures are air dried until no standing moisture is visible. Bound dye is solubilized with 10 mM unbuffered Tris base (pH 10.5) for 5 minutes on a gyratory shaker. OD is read in either a UVmax microtiter plate reader or a Beckman DU-70 spectrophotometer. For maximum sensitivity, OD is measured at 564 nm. Because readings are linear with dye concentrations only below 1.8 OD units, however, suboptimal wavelengths are generally used, so that all samples in an experiment remains within the linear OD range. With most cell lines, wavelengths of approximately 490-530 nm works well for this purpose.(Only for Reference)
分子量 341.84
分子式 C18H20ClN5
CAS No. 885499-61-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 6 mg/mL (17.55 mM)

H2O: <1 mg/mL

DMSO: 25 mg/mL (73.13 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.9253 mL 14.6267 mL 29.2535 mL 73.1336 mL
5 mM 0.5851 mL 2.9253 mL 5.8507 mL 14.6267 mL
10 mM 0.2925 mL 1.4627 mL 2.9253 mL 7.3134 mL
DMSO 20 mM 0.1463 mL 0.7313 mL 1.4627 mL 3.6567 mL
50 mM 0.0585 mL 0.2925 mL 0.5851 mL 1.4627 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Yap TA, et al. Mol Cancer Ther. 2011, 10(2), 360-371.
CYC-116 Sodium salicylate S6K-18 AT7867 PF-4708671 AD80 Pluripotin Vistusertib

相关化合物库

该产品包含在如下化合物库中:
PI3K/Akt/mTOR 化合物库 自噬库 谷氨酰胺代谢化合物库 细胞重编程化合物库 神经再生化合物库 氧化还原化合物库 HIF-1化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

CCT128930 885499-61-6 Autophagy Cytoskeletal Signaling MAPK PI3K/Akt/mTOR signaling Tyrosine Kinase/Adaptors Akt PKA S6 Kinase growth Protein kinase B phosphorylation breast cancer inhibit arrest selective DNA PKB Apoptosis glioblastoma BT474 cell cycle CCT-128930 PTEN Inhibitor U87MG damage CCT 128930 inhibitor

 

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