甲氨蝶呤

(Synonyms: 甲氨蝶呤; Amethopterin; CL14377; WR19039)
目录号: PC78932 纯度: ≥98%
Methotrexate (WR19039) 是一种叶酸类似物,一种二氢叶酸还原酶 DHFR 的抑制剂。Methotrexate 具有抗代谢、抗肿瘤和免疫抑制等活性,常用于类风湿关节炎和多种肿瘤的研究。
CAS No. :59-05-2
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中文名称
甲氨蝶呤
中文别名
6-[[5-氟-2-[(3,4,5-三甲氧基苯基)氨基]-4-嘧啶基]氨基]-2,2-二甲基-2H-吡啶并[3,2-b]-1,4-噁嗪-3(4H)-酮;6-[[5-氟-2-[(3,4,5-三甲氧基苯基)氨基]-4-嘧啶基]氨基]-2,2-二甲基-2H-吡啶并[3,2-B]-1,4-恶嗪-3(4H)-酮;6 - (5 - 氟 - 2 - (3,4,5 - 三甲氧基苯基氨基)-4 - 基氨基)-2-嘧啶,;R-406
英文名称
Methotrexate
英文别名
R-406;6-[5-Fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one;6-[[5-Fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-2H-pyrido[3,2-b]-1,4-oxazin-3(4H)-one;6-[5-Fluoro-2-(3,4,5-trimethoxy-phenylamino)-pyrimidin-4-ylamino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one;R406 (free base);R406;2H-Pyrido[3,2-b]-1,4-oxazin-3(4H)-one, 6-[[5-fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-;6-(5-Fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one;6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one;6-[[5-Fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-2H-pyrido[3,2-b]-1,4-oxazin-3(4H)-one ;R406 Free base;compound 1007;N4-aminocytidine minimum;N4-NH2-Cr;N-Aminocytidine;uridine,4-hydrazone
Cas No.
59-05-2
分子式
C20H22N8O5
分子量
454.44
包装储存
keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
详情描述

Methotrexate (WR19039) 是一种叶酸类似物,一种二氢叶酸还原酶 DHFR 的抑制剂。Methotrexate 具有抗代谢、抗肿瘤和免疫抑制等活性,常用于类风湿关节炎和多种肿瘤的研究。

产品详情
Methotrexate (WR19039) is a folate analog, an inhibitor of the dihydrofolate reductase DHFR. Methotrexate has antimetabolic, antitumor, and immunosuppressive activities, and is commonly used in rheumatoid arthritis and various tumors.
生物活性
方法:6 种儿童白血病和淋巴瘤细胞系 NALM-6、 NALM-16、JURKAT、CEM、RAMOS 和 NAMALWA 用 Methotrexate (0.002-5 μM) 处理 120 h,使用 SRB 方法检测细胞增殖抑制活性。
结果:Methotrexate 对肿瘤细胞的 IC 50 中位数为 78 nM,对六种肿瘤细胞的 IC50 在 33-133 nM 之间。[1]
方法:人卵巢癌细胞 SKOV-3 用 Methotrexate (15-50 μM) 处理 24 h,使用 AO/EtBr probe 检测细胞凋亡情况。
结果:Methotrexate 诱导 SKOV-3 细胞凋亡。[2]
方法:为检测慢性毒性,将 Methotrexate (0.25-6 mg/kg) 腹腔注射给 C57BL/6、DBA/2 和 C3H小鼠,每周五次,持续 12-18 个月。
结果:0.25-2 mg/kg 剂量下的耐受性良好,淋巴组织、睾丸和皮肤中的细胞抑制最小。3-6 mg/kg 剂量下会产生众所周知的急性至亚急性造血和胃肠道损伤,导致早期死亡。[3]
方法:为检测在不同类型风湿性关节炎 (RA) 和多发性硬化症 (MS) 模型中的作用模式,将 Methotrexate (0.1-5 mg/kg) 腹腔注射给不同发病机制的 RA 和 MS 模型,每天一次,持续十四天。
结果:Methotrexate 对 CIA、PIA 等经典 RA 模型及 MS、EAE 模型均有较强的改善作用。Methotrexate 仅在 T 细胞活化之前和依赖于 T 细胞活化的疾病中起作用。[4]
储存方式
keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
参考文献

1.Norris RE, et al. Clinical potency of methotrexate, aminopterin, talotrexin and pemetrexed in childhood leukemias. Cancer Chemother Pharmacol. 2010 May;65(6):1125-30.
2.AlBasher G, et al. Methotrexate-induced apoptosis in human ovarian adenocarcinoma SKOV-3 cells via ROS-mediated bax/bcl-2-cyt-c release cascading. Onco Targets Ther. 2018 Dec 17;12:21-30.
3.Freeman-Narrod M, et al. Chronic toxicity of methotrexate in mice. J Natl Cancer Inst. 1977 Mar;58(3):735-41.
4.Lange F, et al. Methotrexate ameliorates T cell dependent autoimmune arthritis and encephalomyelitis but not antibody induced or fibroblast induced arthritis. Ann Rheum Dis. 2005 Apr;64(4):599-605.

溶解度数据
DMSO: 45 mg/mL (99.02 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 8.3 mg/mL (18.26 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
搜索质检报告(COA)

1.Norris RE, et al. Clinical potency of methotrexate, aminopterin, talotrexin and pemetrexed in childhood leukemias. Cancer Chemother Pharmacol. 2010 May;65(6):1125-30.
2.AlBasher G, et al. Methotrexate-induced apoptosis in human ovarian adenocarcinoma SKOV-3 cells via ROS-mediated bax/bcl-2-cyt-c release cascading. Onco Targets Ther. 2018 Dec 17;12:21-30.
3.Freeman-Narrod M, et al. Chronic toxicity of methotrexate in mice. J Natl Cancer Inst. 1977 Mar;58(3):735-41.
4.Lange F, et al. Methotrexate ameliorates T cell dependent autoimmune arthritis and encephalomyelitis but not antibody induced or fibroblast induced arthritis. Ann Rheum Dis. 2005 Apr;64(4):599-605.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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