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.
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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。 |
靶点 |
|
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 | |
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 |
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 |