Methotrexate-d3
(Synonyms: 甲氨蝶呤 d3) 目录号 : GC47650An internal standard for the quantification of methotrexate
Cas No.:432545-63-6
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
Methotrexate-d3 is intended for use as an internal standard for the quantification of MTX by GC- or LC-MS. MTX is similar in structure to folic acid and aminopterin . It acts by inhibiting the metabolism of folic acid and blocking key enzymes in the synthesis of purines and pyrimidines required for cell proliferation.1,2 MTX is known to induce adenosine release, which mediates many of its anti-inflammatory effects, including the reduction of proinflammatory cytokines.2,3,4 Formulations containing MTX have been used in the treatment of cancer, autoimmune diseases, ectopic pregnancy, and for the induction of medical abortions.5,6 MTX formulations are considered the gold standard of disease-modifying antirheumatic drug (DMARD) therapy to treat both the immune-inflammatory and joint destructive processes of rheumatoid arthritis.7
1.Tian, H., and Cronstein, B.N.Understanding the mechanisms of action of methotrexate: Implications for the treatment of rheumatoid arthritisBull. NYU Hosp. Jt. Dis.65(3)168-173(2007) 2.Swierkot, J., and Szechinski, J.Methotrexate in rheumatoid arthritisPharmacol. Rep.58(4)473-492(2006) 3.Chan, E.S.L., and Cronstein, B.N.Molecular action of methotrexate in inflammatory diseasesArthritis Res.4(4)266-273(2002) 4.Wessels, J.A.M., Huizinga, T.W.J., and Guchelaar, H.J.Recent insights in the pharmacological actions of methotrexate in the treatment of rheumatoid arthritisRheumatology47249-255(2008) 5.Cutolo, M., Sulli, A., Pizzorni, C., et al.Anti-inflammatory mechanisms of methotrexate in rheumatoid arthritisAnn. Rheum. Dis.60(8)729-735(2001) 6.Christin-Maitre, S., Bouchard, P., and Spitz, I.M.Medical termination of pregnancyN. Engl. J. Med.342(13)946-956(2000) 7.Smolen, J.S., and Steiner, G.Therapeutic strategies for rheumatoid arthritisNat. Rev. Drug Dis.2(6)473-488(2003)
| Cas No. | 432545-63-6 | SDF | |
| 别名 | 甲氨蝶呤 d3 | ||
| Canonical SMILES | NC1=NC(N)=C2C(N=CC(CN(C3=CC=C(C(N[C@H](C(O)=O)CCC(O)=O)=O)C=C3)C([2H])([2H])[2H])=N2)=N1 | ||
| 分子式 | C20H19D3N8O5 | 分子量 | 457.5 |
| 溶解度 | DMF: 14 mg/ml,DMSO: 3 mg/ml,PBS (pH 7.2): 1 mg/ml | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1858 mL | 10.929 mL | 21.8579 mL |
| 5 mM | 0.4372 mL | 2.1858 mL | 4.3716 mL |
| 10 mM | 0.2186 mL | 1.0929 mL | 2.1858 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。
Ultrafast selective quantification of methotrexate in human plasma by high-throughput MALDI-isotope dilution mass spectrometry
Bioanalysis 2011 Jun;3(12):1369-78.PMID:21679031DOI:10.4155/bio.11.113.
Background: A new analytical MS method using isotope dilution combined with MALDI-triple quadrupole MS/MS has been developed and validated for the determination of methotrexate and 7-hydroxymethotrexate in plasma. Methotrexate, Methotrexate-d3, 7-hydroxymethotrexate and 7-hydroxymethotrexate-d3 were monitored by selected reaction monitoring using the transitions m/z 455.2→308.2, 458.2→311.2, 471.2→324.2 and 474.2→327.2 for methotrexate, Methotrexate-d3, 7-hydroxymethotrexate and 7-hydroxymethotrexate-d3, respectively. Results: The LLOQ was 1 nmol/l for methotrexate and 7-hydroxymethotrexate while the limit of detection was 0.3 nmol/l for both analytes. The new developed method was cross-validated by a fluorescence polarization immunoassay and tested for its clinical feasibility by measuring plasma samples from patients suffering from acute lymphoblastic leukemia. Plasma methotrexate concentrations ranged between 66.0 and 954 nmol/l and observed 7-hydroxymethotrexate/methotrexate ratios ranged between 0.1 and 32.4, respectively. Conclusion: The new method showed comparable analytical performances as the fluorescence polarization immunoassay, but analyte specificity and sensitivity of the newly developed method were significantly better.
Analysis of mono-, di-, and triphosphates of thioguanosine and methylthioinosine in children with acute lymphoblastic leukemia by LC-MS/MS
J Pharm Biomed Anal 2022 Aug 5;217:114813.PMID:35550492DOI:10.1016/j.jpba.2022.114813.
Mercaptopurine (6-MP) is an indispensable, first-line, drug in the treatment of pediatric acute lymphoblastic leukemia (ALL). However, 6-MP has several intrinsic drawbacks, such as large individual variability in the drug response, undesirable adverse reactions, and drug resistance in patients with release ALL, which requires therapeutic drug monitoring (TDM). Several studies analyzed the total concentration of thiopurine nucleotides in red blood cells (RBCs) after hydrolysis, and two studies detected them separately and accurately by liquid chromatography-tandem mass spectrometry (LC-MS/MS). In this study, we developed a rapid and robust LC-MS/MS method for simultaneous quantitation of mono-, di-, and triphosphates of thioguanosine and methylthioinosine. Not only EDTA and DTT were added, but also EHT1864, a new Rac family small GTPases inhibitor, was innovatively added to ensure the stability of the analytes. Commercial availability and relatively low cost compound Methotrexate-d3 was selected as internal standards. The linearity, accuracy, precision, recovery, matrix effect and stability of the method were all in line with the guidelines. This method provide an accurate and robust new solution for the determination of 6 metabolites of MP in RBCs from ALL patients with maintenance therapy.