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| 品牌 | absin | CAS | 885499-61-6 |
|---|---|---|---|
| 分子式 | C18H20ClN5 | 纯度 | 98% |
| 分子量 | 341.84 | 货号 | abs47028288 |
| 规格 | 2mg | 供货周期 | 现货 |
| 主要用途 | is a potent, ATP-competitive | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
CCT128930 885499-61-6
| 产品描述 | |
| 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. |
| 纯度 | 98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 可溶性/溶解性 | DMSO ：68 mg/mL (198.92 mM) |
| 生物活性 | |
| 靶点 | Akt2 ,p70 S6K ,PKA |
| In vitro(体外研究) | CCT128930 exhibits marked antiproliferative activity against PTEN-deficient human tumor cell lines including U87MG 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 U87MG human glioblastoma cells and Akt pathway blockade. |
| In vivo(体内研究) | CCT128930 at 25 mg/kg i.p. shows a marked antitumor effect in established PTEN-null U87MG 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. |
| 参考文献 | |
| 参考文献 |
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| 研究领域 | |
| 研究领域 | CancerSignal transductionProtein phosphorylationSerine/threonine kinasesAKT CardiovascularAtherosclerosisDiabetes associated CardiovascularHeartCardiac metabolism MetabolismTypes of diseaseDiabetes MetabolismTypes of diseaseHeart disease Signal TransductionProtein PhosphorylationSer / Thr KinasesPKB / AKT Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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