7-hydroxy Methotrexate (sodium salt)
(Synonyms: 7-hydroxy MTX) 目录号 : GC42608
A metabolite of methotrexate
Sample solution is provided at 25 µL, 10mM.
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7-hydroxy Methotrexate (7-hydroxy MTX) is a phase I metabolite of MTX, which is converted by hepatic aldehyde oxidases.[1] Elimination of 7-hydroxy MTX is associated with the multi-drug transporters Abcc2, Abcc3, and Abcg2 in transgenic mouse models. It and the parent compound rapidly accumulate when all three transporters are absent.[2] Formulations containing methotrexate have been used in the treatment of cancer, autoimmune diseases, ectopic pregnancy, and for the induction of medical abortions.[3],[4] Various methods have been described to quantify 7-hydroxy MTX levels during cancer therapy to avoid toxicity.[5],[6]
Reference:
[1]. Johns, D.G., Iannotti, A.T., Sartorelli, A.C., et al. The relative toxicites of methotrexate and aminopterin. Biochem. Pharmacol. 15(5), 555-561 (1966).
[2]. Vlaming, M.L.H., van Esch, A., Pala, Z., et al. Abcc2 (Mrp2), Abcc3 (Mrp3), and Abcg2 (Bcrp1) are the main determinants for rapid elimination of methotrexate and its toxic metabolite 7-hydroxymethotrexate in vivo. Mol. Cancer. Ther. 8(12), 3350-3359 (2009).
[3]. Cutolo, M., Sulli, A., Pizzorni, C., et al. Anti-inflammatory mechanisms of methotrexate in rheumatoid arthritis. Ann. Rheum. Dis. 60(8), 729-735 (2001).
[4]. Christin-Maitre, S., Bouchard, P., and Spitz, I.M. Medical termination of pregnancy. N. Engl. J. Med. 342(13), 946-956 (2000).
[5]. Schofield, R.C., Ramanathan, L.V., Murata, K., et al. Development of an assay for methotrexate and its metabolites 7-hydroxy methotrexate and DAMPA in serum by LC-MS/MS. Methods in Molecular Biology 213-222 (2016).
[6]. Klapkova, E., Kukacka, J., Kotaska, K., et al. The influence of 7-OH methotrexate metabolite on clinical relevance of methotrexate determination. Clin. Lab. 57(7-8), 599-606 (2011).
[1]. Johns, D.G., Iannotti, A.T., Sartorelli, A.C., et al. The relative toxicites of methotrexate and aminopterin. Biochem. Pharmacol. 15(5), 555-561 (1966).
[2]. Vlaming, M.L.H., van Esch, A., Pala, Z., et al. Abcc2 (Mrp2), Abcc3 (Mrp3), and Abcg2 (Bcrp1) are the main determinants for rapid elimination of methotrexate and its toxic metabolite 7-hydroxymethotrexate in vivo. Mol. Cancer. Ther. 8(12), 3350-3359 (2009).
[3]. Cutolo, M., Sulli, A., Pizzorni, C., et al. Anti-inflammatory mechanisms of methotrexate in rheumatoid arthritis. Ann. Rheum. Dis. 60(8), 729-735 (2001).
[4]. Christin-Maitre, S., Bouchard, P., and Spitz, I.M. Medical termination of pregnancy. N. Engl. J. Med. 342(13), 946-956 (2000).
[5]. Schofield, R.C., Ramanathan, L.V., Murata, K., et al. Development of an assay for methotrexate and its metabolites 7-hydroxy methotrexate and DAMPA in serum by LC-MS/MS. Methods in Molecular Biology 213-222 (2016).
[6]. Klapkova, E., Kukacka, J., Kotaska, K., et al. The influence of 7-OH methotrexate metabolite on clinical relevance of methotrexate determination. Clin. Lab. 57(7-8), 599-606 (2011).
| Cas No. | SDF | ||
| 别名 | 7-hydroxy MTX | ||
| 化学名 | N-[4-[[(2,4-diamino-7,8-dihydro-7-oxo-6-pteridinyl)methyl]methylamino]benzoyl]-L-glutamic acid, trisodium salt | ||
| Canonical SMILES | O=C(C(CN(C1=CC=C(C(N([H])[C@@H](CCC(O)=O)C(O)=O)=O)C=C1)C)=N2)N([H])C3=C2C(N)=NC(N)=N3.[Na+].[Na+].[Na+] | ||
| 分子式 | C20H22N8O6•3Na | 分子量 | 539.4 |
| 溶解度 | 3mg/mL in DMSO, 14mg/mL in DMF | 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 | 1.8539 mL | 9.2696 mL | 18.5391 mL |
| 5 mM | 0.3708 mL | 1.8539 mL | 3.7078 mL |
| 10 mM | 0.1854 mL | 0.927 mL | 1.8539 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。
Quality Control & SDS
- View current batch:
- Purity: >96.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet