Everolimus-d4
(Synonyms: RAD001-d4; SDZ-RAD-d4) 目录号 : GC47328An internal standard for the quantification of everolimus
Cas No.:1338452-54-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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)
| 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 |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
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.