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甲氨蝶呤 /Methotrexate {[allProObj[0].p_purity_real_show]}

货号:A103612 同义名: Amethopterin;CL14377

Methotrexate, an antifolate compound, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH and can interfere with the growth of certain cells of the body, especially cells that reproduce quickly, such as cancer cells, bone marrow cells, and skin cells.

Methotrexate 化学结构 CAS号:59-05-2
Methotrexate 化学结构
CAS号:59-05-2
Methotrexate 3D分子结构
CAS号:59-05-2
Methotrexate 化学结构 CAS号:59-05-2
Methotrexate 3D分子结构 CAS号:59-05-2
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Methotrexate 纯度/质量文件 产品仅供科研

货号:A103612 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 DHFR 其他靶点 纯度
Pralatrexate 99%+
Pemetrexed disodium ++++

DHFR, Ki: 7.2 nM

99.9%
Pyrimethamine ++

DHFR, IC50: 15.4 nM

98% HPLC
Pemetrexed ++++

DHFR , Ki: 7.2 nM

99+%
Methotrexate +

hDHFR, IC50: 24 nM

99% (contain ~10%water)
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Methotrexate 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].

Methotrexate 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
NCI-H522 ~1 μM Growth inhibitory assay IC50=229 nM 9022795

Methotrexate 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

Methotrexate 实验方案

计算器
存储液制备 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

Methotrexate 技术信息

CAS号59-05-2
分子式C20H22N8O5
分子量 454.439
别名 Amethopterin;CL14377;NCI-C04671;WR19039
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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

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