PI-103-d8

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PI-103-d8 

PI-103-d8 是 PI-103 的氘代物。PI-103 是一种有效的 PI3K 和 mTOR 抑制剂，抑制 p110α，p110β，p110δ，p110γ，mTORC1 和 mTORC2，IC50 分别为 8 nM，88 nM，48 nM，150 nM，20 nM 和 83 nM。PI-103 还抑制 DNA-PK，IC50

PI-103-d8

PI-103-d8 Chemical Structure

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生物活性

PI-103-d8 is the deuterium labeled PI-103. PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy[1][2][3][4].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

356.40

Formula

C19H8D8N4O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Raynaud FI, et al. Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103through PI-540, PI-620 to the oral agent GDC-0941. Mol Cancer Ther. 2009 Jul;8(7):1725-39.

    [3]. Park S, et al. PI-103, a dual inhibitor of Class IA phosphatidylinositide 3-kinase anLeukemia. 2008 Sep;22(9):1698-706.d mTOR, has antileukemicactivity in AmL. Leukemia. 2008 Sep;22(9):1698-706.

    [4]. López-Fauqued M, et al. The dual PI3K/mTOR inhibitor PI-103 promotes immunosuppression, in vivo tumor growth and increases survival of melanoma cells. Int J Cancer. 2010 Apr 1;126(7):1549-61.

    [5]. Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110 alpha. Cell. 2006 May 19;125(4):733-47.

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