Rapamycin-d3
(Synonyms: 三氘代雷帕霉素,Sirolimus-d3; AY-22989-d3) 目录号 : GC48027An internal standard for the quantification of rapamycin
Cas No.:392711-19-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >≥98% deuterated forms (d1-d3)
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Rapamycin-d3 is intended for use as an internal standard for the quantification of rapamycin by GC- or LC-MS. Rapamycin is an allosteric inhibitor of the mammalian target of rapamycin (mTOR) complex 1 (mTORC1).1 It interacts with FKBP prolyl isomerase 1A (FKBP12) to form a complex that binds to and inhibits the kinase activity of mTORC1. Rapamycin inhibits growth of Rh1 and Rh30 rhabdomyosarcoma cells in serum-free medium, with 50% inhibition observed at concentrations of 0.1 and 0.5 ng/ml, respectively, and increases apoptosis in these cells at 100 ng/ml.2 It also induces autophagy in a variety of cell types.1 Rapamycin inhibits IL-2-induced proliferation of IL-2-dependent T cells by 50% when used at concentrations less than 5 pM.3 Formulations containing rapamycin have been used as immunosuppressive agents in the prevention of organ transplant rejection.
1.Kim, Y.C., and Guan, K.-L.mTOR: A pharmacological target for autophagy regulationJ. Clin. Invest.125(1)25-32(2015) 2.Hosoi, H., Dilling, M.B., Shikata, T., et al.Rapamycin causes poorly reversible inhibition of mTOR and induces p53-independent apoptosis in human rhabdomyosarcoma cellsCancer Res.59(4)886-894(1999) 3.Kay, J.E., Kromwel, L., Doe, S.E.A., et al.Inhibition of T and B lymphocyte proliferation by rapamycinImmunology72(4)544-549(1991)
| Cas No. | 392711-19-2 | SDF | |
| 别名 | 三氘代雷帕霉素,Sirolimus-d3; AY-22989-d3 | ||
| Canonical SMILES | O=C(C(N1[C@H](C(O[C@H]([C@H](C)C[C@@H]2CC[C@@H](O)[C@H](OC)C2)CC([C@H](C)/C=C(C)/[C@@H](O)[C@@H](OC)C([C@@H]3C)=O)=O)=O)CCCC1)=O)[C@]4(O)O[C@H](C[C@H](OC([2H])([2H])[2H])/C(C)=C/C=C/C=C/[C@@H](C)C3)CC[C@H]4C | ||
| 分子式 | C51H76D3NO13 | 分子量 | 917.2 |
| 溶解度 | Chloroform: 5 mg/ml,DMSO: 25 mg/ml,Ethanol: 50 mg/ml,Methanol: 25 mg/ml | 储存条件 | Store at -20°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 | 1.0903 mL | 5.4514 mL | 10.9027 mL |
| 5 mM | 0.2181 mL | 1.0903 mL | 2.1805 mL |
| 10 mM | 0.109 mL | 0.5451 mL | 1.0903 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。
Analytical performance of a new liquid chromatography/tandem mass spectrometric method for determination of everolimus concentrations in whole blood
Ther Drug Monit 2012 Apr;34(2):222-6.PMID:22322402DOI:10.1097/FTD.0b013e318246d515
The immunosuppressant everolimus was recently approved for prophylactic use in the United States, to prevent organ rejection in adult kidney transplant recipients. The currently accepted therapeutic range for everolimus is 3-8 ng/mL. Therapeutic drug monitoring (TDM) using predose EDTA whole blood samples is required to optimize dose. We describe a simple extraction method and analysis by liquid chromatography tandem mass spectrometry (LC-MS/MS) to support routine TDM of everolimus. Samples were prepared by protein precipitation and filtration. The first quadrupole was set to select the ammonium adducts (Equation is included in full-text article.)of everolimus (m/z 975.62) and Rapamycin-d3 (m/z 934.70), the internal standard. The second quadrupole was used as a collision chamber, and the third quadrupole was then used to select characteristic product ions of everolimus (m/z 908.50 and 890.50) and Rapamycin-d3 (m/z 864.60 and 846.50). The method had an analytical measurement range of 2.0-150 ng/mL. Total imprecision, expressed as percent coefficient of variation (mean concentration), was 19.1% (3.3 ng/mL), 10.6% (5.9 ng/mL), 8.1% (19.2 ng/mL), 5.7% (25.8 ng/mL), and 9.1% (34.2 ng/mL). The new method was compared with 2 other everolimus methods also based on LC-MS/MS, with 64 residual patient specimens. Agreement, based on simple linear regression, was excellent. Method A comparison: y = 0.96x - 1.12 (r = 0.99), n = 20, 2.5-44.7 ng/mL. Method B comparison: y = 0.96x + 0.49 (r = 0.99), n = 44, 2.1-85.6 ng/mL. We conclude that this method could support TDM of everolimus for a wide range of clinical indications.