货号:A103612
同义名:
Amethopterin;CL14377
Methotrexate是一种抗叶酸化合物,作为一种非特异性抑制剂,抑制细菌、癌细胞以及正常细胞中的二氢叶酸还原酶(DHFR)。它与DHFR和NADPH形成无活性的三元复合物,干扰某些细胞(尤其是快速分裂的癌细胞、骨髓细胞和皮肤细胞)的生长。
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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 | 活性说明 | 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 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
溶解方案 |
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 |