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Everolimus-d4

(Synonyms: RAD001-d4; SDZ-RAD-d4) 目录号 : GC47328

An internal standard for the quantification of everolimus

Everolimus-d4 Chemical Structure

Cas No.:1338452-54-2

规格 价格 库存
500 μg
¥2,141.00
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1 mg
¥3,854.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

Everolimus-d4 is intended for use as an internal standard for the quantification of everolimus by GC- or LC-MS. Everolimus is a hydroxyethyl ether form of rapamycin that inhibits mTOR signaling through both mTORC1 and mTORC2 when added to cells at 20 nM.1,2 It is orally available and shows improved pharmacokinetics and pharmacodynamics over rapamycin.2 Through its inhibition of mTOR, everolimus inhibits cell proliferation, metabolism, and angiogenesis in certain types of cancer.3,4 It also acts as an immunosuppressive agent in the context of organ transplantation.

1.Zeng, Z., Sarbassov, D.D., Samudio, I.J., et al.Rapamycin derivatives reduce mTORC2 signaling and inhibit AKT activation in AMLBlood109(8)3509-3512(2007) 2.Lebwohl, D., Anak, Ö., Sahmoud, T., et al.Development of everolimus, a novel oral mTOR inhibitor, across a spectrum of diseasesAnn. N.Y. Acad. Sci.129114-32(2013) 3.Yunokawa, M., Koizumi, F., Kitamura, Y., et al.Efficacy of everolimus, a novel mTOR inhibitor, against basal-like triple-negative breast cancer cellsCancer Sci.103(9)1665-1671(2012) 4.Gurk-Turner, C., Manitpisitkul, W., and Cooper, M.A comprehensive review of everolimus clinical reports: A new mammalian target of rapamycin inhibitorTransplantation94(7)659-668(2012)

Chemical Properties

Cas No. 1338452-54-2 SDF
别名 RAD001-d4; SDZ-RAD-d4
Canonical SMILES O=C([C@]1([H])CCCCN1C(C([C@@]2(O)[C@H](C)CC[C@](C[C@H](OC)/C(C)=C/C=C/C=C/[C@H](C3)C)([H])O2)=O)=O)O[C@](CC([C@H](C)/C=C(C)/[C@@H](O)[C@@H](OC)C([C@@H]3C)=O)=O)([H])[C@H](C)C[C@H]4C[C@@H](OC)[C@H](OC([2H])([2H])C([2H])([2H])O)CC4
分子式 C53H79D4NO14 分子量 962.3
溶解度 Chloroform: Soluble,Methanol: Soluble 储存条件 Store at 4°C
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1 mM 1.0392 mL 5.1959 mL 10.3918 mL
5 mM 0.2078 mL 1.0392 mL 2.0784 mL
10 mM 0.1039 mL 0.5196 mL 1.0392 mL
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Research Update

Comparison of a stable isotope-labeled and an analog internal standard for the quantification of everolimus by a liquid chromatography-tandem mass spectrometry method

Ther Drug Monit 2013 Apr;35(2):246-50.PMID:23503452DOI:10.1097/FTD.0b013e318283403e.

Background: Everolimus is an immunosuppressant drug used in solid organ transplantation. Immunoassays and liquid chromatography-mass spectrometry (LC-MS) methods have been used for therapeutic drug monitoring of this drug. In LC-tandem mass spectrometry (MS/MS) methods, both 32-desmethoxyrapamycin and Everolimus-d4 have been used as internal standards. Objectives: To compare 2 internal standards (32-desmethoxyrapamycin and Everolimus-d4) for the quantification of everolimus by an LC-MS/MS method. Methods: Both 32-desmethoxyrapamycin and Everolimus-d4 were introduced in the method validation process with 2 transitions simultaneously monitored for everolimus (975.6 → 908.7 as the quantifier and 975.6 → 926.9 as the qualifier) by an established LC-MS/MS method. The key performance characteristics were lower limit of quantification, accuracy, precision, and comparison with an LC-MS/MS method offered by another laboratory. Results: The lower limit of quantification (LLOQ) was 1.0 ng/mL using either internal standard with an analytical recovery of 98.3%-108.1% across the linear range. The total coefficient of variation for everolimus was 4.3%-7.2% with no significant difference between the 2 internal standards. In comparison with an independent LC-MS/MS method, though Everolimus-d4 offered a better slope (0.95 versus 0.83), both internal standards showed acceptable results and had a coefficient of correlation r > 0.98 in the tested concentration range of 1.2-12.7 ng/mL. Conclusions: Although Everolimus-d4 offered a more favorable comparison with an independent LC-MS/MS method, both Everolimus-d4 and 32-desmethoxyrapamycin had acceptable performance as the internal standards for everolimus quantification by the LC-MS/MS method.

Ultra fast liquid chromatography-tandem mass spectrometry routine method for simultaneous determination of cyclosporin A, tacrolimus, sirolimus, and everolimus in whole blood using deuterated internal standards for cyclosporin A and everolimus

Ther Drug Monit 2010 Feb;32(1):61-6.PMID:20010460DOI:10.1097/FTD.0b013e3181c49a00.

Specific chromatographic methods for the measurement of cyclosporin A, tacrolimus, sirolimus, and everolimus blood levels in patients with organ transplants are time consuming when large numbers of samples must be processed. The authors developed a robust and fast (1 minute) online solid-phase extraction liquid chromatography/tandem mass spectrometry method for the simultaneous quantification of cyclosporin A, tacrolimus, sirolimus, and everolimus. After protein precipitation of the whole blood with zinc sulphate and methanol, the supernatant was loaded on a wide pore reversed-phase column and cleansed of potential interferences with high flow for 20 seconds. After column switching, the analytes were transferred within 20 seconds in the back-flush mode to a short phenyl-hexyl column. The valve was then returned to its initial position and the chromatographic separation performed within 20 seconds. In the meantime, the loading column was prepared for the next injection. Ammoniated adducts of protonated molecules were used as precursor ions for all analytes. Multiple-reaction mode transitions for each immunosuppressant and the internal standards were used for quantification. The working range of the method was 10-1500 microg/L for cyclosporin A, 1.0-44 microg/L for tacrolimus, 1.0-48 microg/L for sirolimus, and 1.2-48 microg/L for everolimus. Within and between-run assay coefficients of variation ranged from 1.8% to 13.0%. The described liquid chromatography/tandem mass spectrometry method shows best performance using the internal standards cyclosporin A-d4 for cyclosporin A, Everolimus-d4 for everolimus and ascomycin for tacrolimus and sirolimus. In conclusion, the authors present a very fast, robust, and economical analytical method for therapeutic monitoring of multiple immunosuppressants in daily clinical practice.