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产品介绍
产品介绍
产品信息
抗原名称
Akt1 ,Akt2 ,Akt3 ,ROCK2
商品描述
AZD5363有效抑制Akt(Akt1/Akt2/3)的所有亚型，在无细胞试验中IC50为3 nM/8 nM/8 nM，对P70S6K/PKA也具有相似的抑制效果，而对ROCK1/2抑制活性较低。
分子量
428.92
纯度
98% min
可溶性
DMSO Solubility: 86 mg/mL (200.5 mM)
In vitro(体外研究)
AZD5363 is a potent Akt inhibitor with IC50 of 3 nM, 8 nM and 8 nM for Akt1, Akt2 and Akt3, respectively. AZD5363 inhibits phosphorylation of AKT substrates in cells with a potency of approximately 0.3 to 0.8 μM. AZD5363 inhibits the proliferation of 41 of 182 solid and hematologic tumor cell lines with a potency of Activating mutations in PIK3CA, loss or inactivation of tumor suppressor PTEN, or HER2 amplification all are significantly predictive of responsiveness to AZD5363. Additionally, correlation is also seen between the RAS mutation status of cell lines and resistance to AZD5363.
In vivo(体内研究)
Oral dosing of AZD5363 (100, 300 mg/kg) to nude mice causes dose- and time-dependent reduction of PRAS40, GSK3β, and S6 phosphorylation in BT474c xenografts, reversible increases in blood glucose concentrations, and dose-dependent decreases in 2fluoro-2-deoxy-d-glucose (18F-FDG) uptake in U87-MG xenografts. Chronic oral dosing of AZD5363 (130, 200, and 300 mg/kg) causes dose-dependent growth inhibition of xenografts derived from various tumor types, including HER2+ breast cancer models that are resistant to trastuzumab. AZD5363 also significantly enhances the antitumor activity of docetaxel, lapatinib, and trastuzumab in breast cancer xenografts.
背景
别名
AZD-5363; AZD 5363
分子式
C21H25ClN6O2
CAS号
1143532-39-1
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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