甲氨蝶呤作用机制 - Medchemexpress - MCE中国

1、Product Data SheetMethotrexateCat. No.: HY-14519CAS No.: 59-05-2分式: CHNO分量: 454.44作靶点: Antifolate; ADC Cytotoxin; Apoptosis作通路: Cell Cycle/DNA Damage; Antibody-drug Conjugate/ADC Related; Apoptosis储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性数据体外实验 D

2、MSO : 50 mg/mL (110.03 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 2.2005 mL 11.0026 mL 22.0051 mL5 mM 0.4401 mL 2.2005 mL 4.4010 mL10 mM 0.2201 mL 1.1003 mL 2.2005 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C

3、, 1 month (protect from light)。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 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 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineS

4、olubility: 2.5 mg/mL (5.50 mM); Clear solution此案可获得 2.5 mg/mL (5.50 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.50 mM); Clear solution此案可获得 2

5、.5 mg/mL (5.50 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合Page 1 of 2 www.MedChemE均匀。BIOLOGICAL ACTIVITY物活性 Methotrexate (Amethopterin)种抗代谢物和抗叶酸药物，可抑制氢叶酸还原酶，从防叶酸转化为四氢叶酸并抑制 DNA 合成。Methotrexate (Amethopterin) 世界上多数国家/地区治疗类风湿性关节炎的选抗疾病风湿病药物 (DMARD)，并且 抗肿瘤药，可于

6、对抗多种不同的癌症，例如急性淋巴细胞病和实体癌123。IC & Target Traditional Cytotoxic Agents体外研究 Methotrexate (MTX), which has a more predictable toxicity profile than aminopterin, has become a cornerstone of thetreatment for childhood acute lymphoblastic leukemia (ALL) and for non-Hodgkins lymphoma1.体内研究 Methotrexate (MTX)

7、 exposure reduces thymus and spleen indices of mice. Methotrexate markedly decreases whiteblood cells, thymic and splenic lymphocytes at dose 5 mg/kg. However, there is a significant difference between thetreatment plus control group and the model group (p0.01). The combination of grape seed proanth

8、ocyanidins andSiberian ginseng eleutherosides obviously diminishes the effects of Methotrexate exposure on indices of thymus andspleens in mice2.PROTOCOLCell Assay 1 Each cell line is studied in growth inhibition experiments using 96-well microtiter plates. As antifols are scheduledependent, prelimi

9、nary experiments are aimed at defining the longest duration of exposure that would allow forcontinuous logarithmic phase growth of cells without changing of the culture media while maintaining a linearrelationship between SRB optical density and cell number. Twenty-four hours after cell plating, the

10、 cell lines areexposed to the antifol for 120 h (three replicates per experiment). To ensure that a complete sigmoidal survival-concentration curve could be observed, the following drug concentrations are studied: Methotrexate (0.002-5 M),AMT (0.0001-1 M), PXD (0.0003-10 M), TLX (0.0002-0.5 M). Expe

11、riments are repeated at least twice1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice2Administration 2 The combination of bioactive phytochemicals is administered one week prior to the Methotrexate exposure.Treatment group I: mice are given a

12、 combination of green tea polyphenols and eleutherosides from Siberian ginseng(0.2 mL/10 g, i.g. once daily) for 15 days, and a single dose of Methotrexate (2 mg/kg, i.p. once daily) is added on the8th day. Treatment group II: mice are given a combination of grape seed proanthocyanidins and eleuther

13、osides fromSiberian ginseng for 15 days, and Methotrexate is administered on the 8th day in a similar manner. Model group:animals received distilled water instead of bioactive phytochemicals combinations for 15 days and the sameMethotrexate protocol applied to this group on the 8th day. Control grou

14、p: mice are given distilled water through 15days and physiological saline instead of Methotrexate is administered on the 8th day in a similar manner. Twelvehours after the final doses, the animals are euthanized by cervical dislocation.MCE has not independently confirmed the accuracy of these method

15、s. They are for reference only.户使本产品发表的科研献 Cancers (Basel). 2019 Oct 25;11(11). pii: E1654.Page 2 of 3 www.MedChemE J Mol Med (Berl). 2019 Aug;97(8):1183-1193. J Biol Chem. 2019 Dec 27;294(52):20084-20096. Sci Rep. 2018 Jun 21;8(1):9472. Acta Pharmacol Sin. 2020 May 12.See more customer validations

16、on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Tian H, et al. Understanding the mechanisms of action of methotrexate: implications for the treatment of rheumatoid arthritis. Bull NYU Hosp Jt Dis.2007;65(3):168-73.2. Swierkot J, et al. Methotrexate in rheumatoid arthritis. Pharmacol Rep. 2006 Jul-Aug;58(4):473-92.3. Ehab Tousson, et al. The Effect of L-carnitine on Amethopterin-induced Toxicity