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Rapamycin-d3

(Synonyms: 三氘代雷帕霉素,Sirolimus-d3; AY-22989-d3) 目录号 : GC48027

An internal standard for the quantification of rapamycin

Rapamycin-d3 Chemical Structure

Cas No.:392711-19-2

规格 价格 库存 购买数量
500 μg
¥1,525.00
现货
1 mg
¥2,295.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

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)

Chemical Properties

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
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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
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Research Update

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.