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CCT128930
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CCT128930
CAS No. : 885499-61-6
MCE 站:CCT128930
产品活性:CCT128930 是一种有效的选择性 Akt2 抑制剂 (IC50 为 6 nM),比作用于 PKA 激酶 (IC50 为 168 nM) 选择性高 28 倍,比作用于 p70S6K (IC50 为 120 nM) 选择性高 20 倍。
研究领域:PI3K/Akt/mTOR | Autophagy
In Vitro: CCT128930 exhibits marked antiproliferative activity and inhibits the phosphorylation of a range of Akt substrates in multiple tumor cell lines in vitro, consistent with Akt inhibition. CCT128930 causes a G1 arrest in PTEN-null U87MG human glioblastoma cells, consistent with Akt pathway blockade. CCT128930 is a potent ATP-competitive Akt inhibitor, which is initially screened at 10 ?M against a panel of kinases representative of the human protein kinome. In view of the potential of ATP-competitive inhibitors to cross-react with the closely related AGC class of kinases, the IC50 of CCT128930 against selected AGC kinases is determined. The GI50 values of CCT128930 for growth inhibition are 6.3 μM±2.2 (n=3) for U87MG human glioblastoma cells, 0.35 μM±0.11 (n=4) for LNCaP human prostate cancer cells, and 1.9 μM±0.80 (n=5) for PC3 human prostate cancer cells, all of which are PTEN-deficient human tumor cell lines.
In Vivo: The pharmacokinetics of CCT128930 after a single dose of 25 mg/kg are shown. Following i.v. administration, CCT128930 reaches a peak concentration of 6.4 ?M in plasma and is eliminated with a relatively short half-life, high volume of distribution and rapid clearance, giving an AUC0-∞ of 4.6 ?Mh. Following i.p. administration, the peak plasma drug concentration is 4-fold lower and the plasma clearance is similar to that observed i.v..The corresponding AUC0-∞ is 1.3 ?Mh, giving an i.p. bioavailability of 29%.
相关产品:Bioactive Compound Library Plus | Kinase Inhibitor Library | PI3K/Akt/mTOR Compound Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Differentiation Inducing Compound Library | Oxygen Sensing Compound Library | Glycolysis Compound Library | Cytoskeleton Compound Library | Glutamine Metabolism Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Honokiol | GSK-690693 | Artemisinin | Oridonin | Perifosine | Guggulsterone | Miransertib | Triciribine | Recilisib | SU6656 | Isobavachalcone | Scutellarin | Deguelin | Miltefosine | A-674563 hydrochloride | α-Linolenic acid | YS-49 | Urolithin B | Polyphyllin I | Pachymic acid | 3CAI | 1,3-Dicaffeoylquinic acid | Esculetin | Cyclovirobuxine D | Licochalcone E | SC66 | Akt1 and Akt2-IN-1 | Arnicolide D | Loureirin A
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