Everolimus-d4(Synonyms: RAD001-d4; SDZ-RAD-d4)

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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、同位素标记物，专注于信号通路和疾病研究领域。
Everolimus-d4 (Synonyms: RAD001-d4; SDZ-RAD-d4)

Everolimus-d4 (RAD001-d4) 是 Everolimus 的氘代物。Everolimus (RAD001) 是一种 Rapamycin 的衍生物，也是一种有效的，选择性的和口服活性的 mTOR1 抑制剂。Everolimus 与 FKBP-12 结合可产生免疫抑制复合物。Everolimus 抑制肿瘤细胞增殖并诱导细胞凋亡 (apoptosis) 和自噬 (autophagy)。Everolimus 具有有效的免疫抑制和抗癌活性。

Everolimus-d4(Synonyms: RAD001-d4; SDZ-RAD-d4)

Everolimus-d4 Chemical Structure

CAS No. : 1338452-54-2

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生物活性

Everolimus-d4 (RAD001-d4) is the deuterium labeled Everolimus. Everolimus (RAD001) is a Rapamycin derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities[1][2].

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

962.25

Formula

C53H79D4NO14
CAS 号

1338452-54-2
中文名称

依维莫司 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]. O’Reilly T, et al. Biomarker Development for the Clinical Activity of the mTOR Inhibitor Everolimus (RAD001): Processes,Limitations, and Further Proposals. Transl Oncol. 2010 Apr;3(2):65-79.

    [3]. Kawata T, et al. Dual inhibition of the mTORC1 and mTORC2 signaling pathways is a promising therapeutic target for adult T-cell leukemia. Cancer Sci. 2018 Jan;109(1):103-111.

    [4]. Lane HA, et al. mTOR inhibitor RAD001 (everolimus) has antiangiogenic/vascular properties distinct from a VEGFR tyrosine kinase inhibitor. Clin Cancer Res, 2009, 15(5), 1612-1622.

    [5]. Zhu Y, et al. Antitumor effect of the mTOR inhibitor Everolimus on human breast cancer stem cells in vitro and in vivo. Tumour Biol. 2012 Oct;33(5):1349-62.

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