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Methotrexate

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Chemical Structure| 59-05-2 同义名 : Amethopterin;CL14377;NCI-C04671;WR19039
CAS号 : 59-05-2
货号 : A103612
分子式 : C20H22N8O5
纯度 : 99% (contain ~10%water)
分子量 : 454.439
MDL号 : MFCD00064370
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(110.03 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 3.9 mg/mL clear

PO 0.5% CMC-Na 80 mg/mL suspension

生物活性
靶点

  • DHFR

    hDHFR, IC50:24 nM
描述 Methotrexate (MTX) is used as an anchor disease-modifying anti-rheumatic drugs (DMARDs) in treating rheumatoid arthritis (RA) because of its potent efficacy and tolerability[3]. Methotrexate is a well-tolerated and effective treatment for allergic contact dermatitis, and shows comparable efficacy to immunomodulatory agents such as cyclosporine and azathioprine, with robust efficacy despite persistent allergen exposure in patients with allergic contact dermatitis[4]. The intrathecal administration of methotrexate can provide therapeutic concentrations in the cerebrospinal fluid (CSF) without the use of high-dose intravenous methotrexate[5]. Formulation consisting prefilled syringe with high concentration of MTX and pre-attached needleis especially suitable for methotrexate subcutaneousself-administration[6]. The dose and duration of MTX therapy for EP (Ectopic pregnancy) is much lower than that used in oncology cases, thus reducing side effects and increasing safety[7].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
MCF7-ADR ~1 μM Growth inhibitory assay IC50=78 nM 9022795
NCI-H23 ~1 μM Growth inhibitory assay IC50=43 nM 9022795
NCI-H460 ~1 μM Growth inhibitory assay IC50=28 nM 9022795
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

11.00mL

2.20mL

1.10mL

22.01mL

4.40mL

2.20mL
参考文献

[1]Wang W, Zhou H, Liu L. Side effects of methotrexate therapy for rheumatoid arthritis: A systematic review. Eur J Med Chem. 2018 Oct 5;158:502-516

[2]Patel A, Burns E, Burkemper NM. Methotrexate use in allergic contact dermatitis: a retrospective study. Contact Dermatitis. 2018 Mar;78(3):194-198

[3]Nelson RW, Frank JT. Intrathecal methotrexate-induced neurotoxicities. Am J Hosp Pharm. 1981 Jan;38(1):65-8

[4]Szczerkowska-Dobosz A. [Subcutaneous methotrexate in psoriasis and psoriatic arthritis treatment]. Wiad Lek. 2016;69(4):675-679. Polish

[5]Barnhart K, Coutifaris C, Esposito M. The pharmacology of methotrexate. Expert Opin Pharmacother. 2001 Mar;2(3):409-17