Olaparib-d4-1(Synonyms: AZD2281-d4-1; KU0059436-d4-1)

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Olaparib-d4-1 (Synonyms: AZD2281-d4-1; KU0059436-d4-1)

Olaparib-d4-1 (AZD2281-d4-1) 是 Olaparib 的氘代物。Olaparib (AZD2281; KU0059436) 是一种口服有效的 PARP 抑制剂，抑制 PARP-1 和 PARP-2 的 IC50 分别为 5 和 1 nM。Olaparib 是一种自噬 (autophagy) 和线粒体自噬 (mitophagy) 激活剂。

Olaparib-d4-1(Synonyms: AZD2281-d4-1; KU0059436-d4-1)

Olaparib-d4-1 Chemical Structure

CAS No. : 2143107-55-3

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生物活性

Olaparib-d4-1 (AZD2281-d4-1) is the deuterium labeled Olaparib. Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

438.49

Formula

C24H19D4FN4O3
CAS 号

2143107-55-3
中文名称

奥拉帕尼 d4
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]. Menear KA, et al. 4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1. J Med Chem. 2008 Oct 23;51(20):6581-91

    [3]. Senra JM, et al. Inhibition of PARP-1 by olaparib (AZD2281) increases the radiosensitivity of a lung tumor xenograft.Mol Cancer Ther. 2011 Oct;10(10):1949-58.

    [4]. Yasukawa M, et al. Synergetic Effects of PARP Inhibitor AZD2281 in Oral Squamous Cell Carcinoma in Vitro and in Vivo. Int J Mol Sci. 2016 Feb 24;17(3):272.

    [5]. Bian X, et al. PTEN deficiency sensitizes endometrioid endometrial cancer to compound PARP-PI3K inhibition but not PARP inhibition as monotherapy. Oncogene. 2018 Jan 18;37(3):341-351.

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