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。
HazMat Fee + There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
| Type | HazMat fee for 500 gram (Estimated) |
| Excepted Quantity | USD 0.00 |
| Limited Quantity | USD 15-60 |
| Inaccessible (Haz class 6.1), Domestic | USD 80+ |
| Inaccessible (Haz class 6.1), International | USD 150+ |
| Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |


| 规格 | 价格 | 会员价 | 库存 | 数量 | |||
|---|---|---|---|---|---|---|---|
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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% | |||||||||||||||||
| 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]. |
| Concentration | Treated Time | Description | References | |
| Ramos cells | 20 μM | 72 hours | To investigate the effect of FTCD depletion on methotrexate sensitivity, results showed that FTCD depletion significantly reduced the sensitivity of Ramos cells to methotrexate | Nature. 2018 Jul;559(7715):632-636 |
| HEL cells | 5 μM | 3 days | To investigate the effect of FTCD depletion on methotrexate sensitivity, results showed that FTCD depletion significantly reduced the sensitivity of HEL cells to methotrexate | Nature. 2018 Jul;559(7715):632-636 |
| BHK-CD16a | 10 μM | Used for culturing BHK-CD16a cells to study ADCC activity of CD19 antibodies | Front Immunol. 2022 Aug 31;13:957874. | |
| BT-474 cells | 0.1 µM | 72 h | MTX treatment increases the intracellular concentration of the metabolite AICAR, resulting in AMPK activation. Methotrexate-induced AMPK activation leads to decreased one-carbon metabolism gene expression and cellular proliferation as well as increased global bioenergetic capacity. | Sci Rep. 2020 May 12;10(1):7838. |
| mouse embryonic fibroblasts (MEFs) | 0.1 µM | 72 h | MTX caused a strong increase (~30 fold) in endogenous AICAR levels in breast cancer cells and mouse embryonic fibroblasts (MEFs) | Sci Rep. 2020 May 12;10(1):7838. |
| A549 cells | 1 μM | To investigate the effects of MTX on Th17 cell differentiation, results showed that MTX-treated A549 cells co-cultured with PBMCs significantly increased the frequency of Th17 cells. | EBioMedicine. 2024 Oct;108:105339. | |
| Molt4 cells | 90 nM | To evaluate the synergy between methotrexate and SHIN2, results showed that methotrexate increased sensitivity to SHIN2 | Leukemia. 2021 Feb;35(2):377-388. |
| Administration | Dosage | Frequency | Description | References | ||
| C57BL/6 nude mice | Acute lymphoblastic leukemia mouse model | Intraperitoneal injection | 80 mg/kg ginger extract and 5 mg/kg MTX | Five times a week for ginger extract and once a week for MTX, lasting two months | To evaluate the anti-leukemic activity of ginger extract alone or in combination with MTX on ALL mouse models, results showed that combined treatment significantly increased survival rate and reduced damages in brain and liver tissues. | J Cell Mol Med. 2021 May 3;25(13):6148–60 |
| DBA/1J mice | Collagen-induced arthritis (CIA) mouse model | Intraperitoneal injection | 23 mg/kg | Thrice a week for 38 days | To evaluate the effect of MTX on arthritis in CIA mice, the results showed that MTX significantly alleviated arthritis symptoms in CIA mice. | Clin Transl Med. 2022 Dec;12(12):e1148. |
| DBA/1J female mice | Bovine collagen-induced arthritis (CIA) model | Intragastric administration | 0.92 mg/kg | Twice a week for 30 days | To evaluate the therapeutic effect of Methotrexate on arthritis in CIA mice, the results showed that Methotrexate was effective in controlling inflammation but had no obvious benefits in regulating weight loss and mechanical allodynia | Front Pharmacol. 2021 May 28;12:693777 |
| DBA/1 mice | Collagen-induced arthritis (CIA) model | Oral gavage | 2 mg/kg | Every 3 days for 20 days | To evaluate the therapeutic effect of MTX on CIA model mice, the results showed that MTX significantly alleviated arthritis symptoms and footpad swelling. | Front Immunol. 2018 Nov 27;9:2762 |
| SKG mice | RA-ILD model | Intraperitoneal injection | 7.5 mg/kg | Twice weekly for 12 weeks | To investigate the effects of MTX on pulmonary inflammation in the RA-ILD mouse model, results showed that MTX exacerbated pulmonary inflammation, increased immune cell infiltration, and fibrosis. | EBioMedicine. 2024 Oct;108:105339. |
| Mice | NOTCH1-driven mouse primary T-ALL model | Intraperitoneal injection | 10 mg/kg | Administered every 5 days for 4 weeks | To evaluate the synergy between methotrexate and SHIN2, results showed that the combination significantly extended mouse survival | Leukemia. 2021 Feb;35(2):377-388. |
| 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 | 454.44 |
| SMILES Code | O=C(O)[C@@H](NC(C1=CC=C(N(CC2=NC3=C(N)N=C(N)N=C3N=C2)C)C=C1)=O)CCC(O)=O |
| MDL No. | MFCD00064370 |
| 别名 | Amethopterin; CL14377; NCI-C04671; WR19039 |
| 运输 | 蓝冰 |
| InChI Key | FBOZXECLQNJBKD-ZDUSSCGKSA-N |
| Pubchem ID | 126941 |
| 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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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