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

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+
Methotrexate/甲氨蝶呤 化学结构 CAS号:59-05-2
Methotrexate/甲氨蝶呤 化学结构
CAS号:59-05-2
Methotrexate/甲氨蝶呤 3D分子结构
CAS号:59-05-2
Methotrexate/甲氨蝶呤 化学结构 CAS号:59-05-2
Methotrexate/甲氨蝶呤 3D分子结构 CAS号:59-05-2
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Methotrexate/甲氨蝶呤 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%
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/甲氨蝶呤 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/甲氨蝶呤 细胞实验

Cell Line
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.

Methotrexate/甲氨蝶呤 动物实验

Species
Animal Model
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.

Methotrexate/甲氨蝶呤 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/甲氨蝶呤 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/甲氨蝶呤 技术信息

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

请根据您的动物给药指南选择适当的溶解方案。
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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