Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CCT128930 hydrochloride (CCT128930 hydrochloride) 是一种选择性 AKT 抑制剂,具有抗肿瘤活性。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。
规格 | 价格/CNY | 货期 | 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 * 10 mM (in DMSO) | ¥ 979 | 现货 |
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 | p70 S6K:120 nM, PKA:168 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) |
分子量 | 378.3 |
分子式 | C18H21Cl2N5 |
CAS No. | 2453324-32-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (145.39 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6434 mL | 13.217 mL | 26.434 mL | 66.0851 mL |
5 mM | 0.5287 mL | 2.6434 mL | 5.2868 mL | 13.217 mL | |
10 mM | 0.2643 mL | 1.3217 mL | 2.6434 mL | 6.6085 mL | |
20 mM | 0.1322 mL | 0.6609 mL | 1.3217 mL | 3.3043 mL | |
50 mM | 0.0529 mL | 0.2643 mL | 0.5287 mL | 1.3217 mL | |
100 mM | 0.0264 mL | 0.1322 mL | 0.2643 mL | 0.6609 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
CCT128930 hydrochloride 2453324-32-6 Apoptosis Autophagy Cytoskeletal Signaling PI3K/Akt/mTOR signaling Tyrosine Kinase/Adaptors Akt PKA mTOR U87MG cell CCT128930 hydrochloride(885499-61-6 Free base) phosphorylation selective DNA damage CCT128930 glioblastoma arrest CCT 128930 Hydrochloride breast cancer Inhibitor BT474 PTEN growth CCT-128930 Hydrochloride CCT128930 Hydrochloride PKB inhibit CCT 128930 CCT-128930 hydrochloride cycle CCT-128930 Protein kinase B inhibitor