TAS-117 hydrochloride
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产品名称:
TAS-117 hydrochloride
产品型号:
GOY-Y2839
产品展商:
谷研
产品文档:
无相关文档
发布时间:2023-05-04
简单介绍
TAS-117 hydrochlorideDMSO : 62.5 mg/mL (135.59 mM; ultrasonic and warming and heat to 60°C)
TAS-117 hydrochloride
的详细介绍
性能参数
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产品名称
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TAS-117 hydrochloride
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规格
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5 mg 10 mg 25 mg
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货号
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GOY-Y2839
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含量
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>98.00%
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CAS
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N/A
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别名
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N/A
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化学名
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N/A
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分子式
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C26H25ClN4O2
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分子量
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分子量 460.96
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溶解度
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DMSO : 62.5 mg/mL (135.59 mM; ultrasonic and warming and heat to 60°C)
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储存条件
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Store at -20°C
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General tips
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用途
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仅供科研
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价格
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电询
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详细内容
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TAS-117 hydrochloride is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). TAS-117 hydrochloride triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. TAS-117 hydrochloride induces apoptosis and autophagy[1].
TAS-117 (1 μM; 6 hours) blocks basal phosphorylation of Akt and downstream p-FKHR/FKHRL1 in MM cells with high baseline p-Akt[1].TAS-117 (0-10 μM; 72 hours) selectively inhibits Akt and induces cytotoxicity in MM cells with high baseline phosphorylation of Akt[1].TAS-117 abrogates the cytoprotective effect of the bone marrow microenvironment associated with Akt inhibition in both MM cells and BMSCs. TAS-117 enhances Carfilzomib-induced cytotoxicity and fatal ER stress in MM cells. TAS-117 (0.5, 1 μM) triggers G0/G1 arrest followed by apoptosis, associated with induction of autophagy and endoplasmic reticulum stress response[1].TAS-117 enhances bortezomib-induced cytotoxicity, associated with increased CHOP (a fatal ER-stress marker) and PARP cleavage and blockade of bortezomib-induced p-Akt, suggesting that TAS-117 augments Bortezomib-induced ER stress and apoptotic signaling[1].
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