Methotrexate disodium
(Synonyms: 甲氨蝶呤二钠盐,Amethopterin disodium; CL14377 disodium; WR19039 disodium) 目录号 : GC61047
Methotrexate sodium, an inhibitor of tetrahydrofolate dehydrogenase, is an antineoplastic antimetabolite with immunosuppressant properties.
Cas No.:7413-34-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Methotrexate sodium, an inhibitor of tetrahydrofolate dehydrogenase, is an antineoplastic antimetabolite with immunosuppressant properties.
Methotrexate (0.1-10 mM) induces apoptosis of in vitro activated T cells from human peripheral blood. Methotrexate achieves clonal deletion of activated T cells in mixed lymphocyte reactions. Methotrexate can selectively delete activated peripheral blood T cells by a CD95-independent pathway. [1] Methotrexate is taken up by cells via the reduced folate carrier and then is converted within the cells to polyglutamates. Methotrexate leads to diminished production of leukotriene B4 by neutrophils stimulated ex vivo. Methotrexate polyglutamates inhibit the enzyme aminoimidazolecarboxamidoadenosineribonucleotide (AICAR) transformylase more potently than the other enzymes involved in purine biosynthesis. Methotrexate is also known to suppress TNF activity by suppressing TNF-induced nuclear factor-κB activation in vitro, in part related to a reduction in the degradation and inactivation of an inhibitor of this factor, IκBα, and probably related to the release of adenosine. Methotrexate suppresses the production of both TNF and IFN-γ by T-cell-receptor-primed T lymphocytes from both healthy human donors and RA patients. Methotrexate treatment is associated with a significant decrease of TNF-α-positive CD4+ T cells, while the number of T cells expressing the anti-inflammatory cytokine IL-10 increased. [2]
Methotrexate increases splenocyte AICAR content, raised adenosine concentrations in exudates from carrageenan-inflamed air pouches, and markedly inhibits leukocyte accumulation in inflamed air pouches in mice. Methotrexate-mediated reduction in leukocyte accumulation is partially reversed by injection of adenosine deaminase (ADA) into the air pouch, completely reverses by a specific adenosine A2 receptor antagonist, 3,7-dimethyl-1-propargylxanthine (DMPX), but not affected by an adenosine A1 receptor antagonist, 8-cyclopentyl-dipropylxanthine in mice. [3]
[1] Genestier L, et al. J Clin Invest, 1998, 102(2), 322-328. [2] Chan ES, et al. Arthritis Res, 2002, 4(4), 266-273. [3] Cronstein BN, et al. J Clin Invest, 1993, 92(6), 2675-2682.
| Cas No. | 7413-34-5 | SDF | |
| 别名 | 甲氨蝶呤二钠盐,Amethopterin disodium; CL14377 disodium; WR19039 disodium | ||
| Canonical SMILES | NC1=NC(N)=C2C(N=CC(CN(C)C3=CC=C(C(N[C@@H](CCC(O[Na])=O)C(O[Na])=O)=O)C=C3)=N2)=N1 | ||
| 分子式 | C20H20N8Na2O5 | 分子量 | 498.4 |
| 溶解度 | Water : 99mg/mL | 储存条件 | 4°C, away from moisture and light |
| General tips | 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0064 mL | 10.0321 mL | 20.0642 mL |
| 5 mM | 0.4013 mL | 2.0064 mL | 4.0128 mL |
| 10 mM | 0.2006 mL | 1.0032 mL | 2.0064 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Selective Cell Penetrating Peptide-Functionalized Polymersomes Mediate Efficient and Targeted Delivery of Methotrexate disodium to Human Lung Cancer In Vivo
Adv Healthc Mater 2018 Apr;7(7):e1701135.PMID:29280317DOI:10.1002/adhm.201701135.
It is a long challenge to develop nanomedicines that simultaneously possess tumor cell selectivity and penetration functions. Here, it is reported that selective cell penetrating peptide (RLWMRWYSPRTRAYGC)-functionalized polymersomes (SCPP-PS) mediate efficient and targeted delivery of Methotrexate disodium (MTX) to human lung cancer in vivo. SCPP-PS with an SCPP density of 18.7% is self-crosslinked, has a small size (63-65 nm), and high MTX loading (up to 19.4 wt%), shows selective uptake and fast penetration into A549 lung cancer cells, and efficiently releases MTX intracellularly. Interestingly, MTX-loaded SCPP-PS (MTX-SCPP-PS) displays much lower IC50 than those of MTX-PS and free MTX. Installing SCPP to polymersomes has no detrimental effect to their long blood circulation time but significantly increases drug accumulation in A549 tumor (5.3% injected dose per gram at 8 h post injection). Remarkably, SCPP-PS exhibits deep penetration in to A549 tumors. MTX-SCPP-PS completely inhibits tumor progression and significantly improves survival rates in mice bearing A549 lung tumor xenografts as compared to MTX-PS and free MTX groups (median survival time: 75 vs 45 and 38 d, respectively), without causing noticeable adverse effects. These results highlight that functionalization of nanomedicines with SCPP is a feasible strategy to achieve efficient and targeted tumor therapy.
Preparation of nanoscale cationic metal-organic framework Nano Mn(III)-TP for theranostics based on valence changes
J Mater Chem B 2022 Nov 9;10(43):8988-8995.PMID:36314257DOI:10.1039/d2tb01619b.
A single treatment strategy to produce a significant effect on cancer treatment is difficult due to the complex variability of the tumor environment. Herein, considering over-expressed glutathione (GSH) in the tumor environment can reduce Mn3+ to Mn2+, and Mn2+ exhibits an excellent T1-weighted magnetic resonance imaging performance and a good Fenton-like effect. A Mn-based nano-cation metal-organic framework (MOF) with a size of about 200 nm was synthesized and labeled as Nano Mn(III)-TP. It showed an outstanding T1-weighted MRI performance and Fenton-like effect due to valence changes of the Mn ions. Meanwhile, MTXNa@Nano Mn(III)-TP was obtained by loading with the anionic anticancer drug Methotrexate disodium (MTXNa), and it could release MTXNa specifically in GSH solution with different pH values and temperatures, resulting in an improvement in the tumor suppressive effect of the Nano Mn(III)-TP. Based on the nanoplatform, the effective combination of magnetic resonance imaging (MRI), CDT and chemotherapy could be used as a potential therapeutic agent for multimodal therapy, which is also expected to be applied to clinical tumor treatment.
Efficient and Targeted Suppression of Human Lung Tumor Xenografts in Mice with Methotrexate Sodium Encapsulated in All-Function-in-One Chimeric Polymersomes
Adv Mater 2016 Oct;28(37):8234-8239.PMID:27383234DOI:10.1002/adma.201600065.
Anisamide-functionalized reversibly crosslinked chimeric polymersomes emerge as an "all-function-in-one" nanoplatform for efficient loading and targeted delivery of Methotrexate disodium, a potent water-soluble anticancer drug, to sigma receptor overexpressing H460 nonsmall lung cancer xenografts in vivo, leading to markedly improved tumor-growth inhibition and survival rate and depleted adverse effects as compared to the clinically used formulation (Trexall).
Quantification of drugs encapsulated in liposomes by 1H NMR
Colloids Surf B Biointerfaces 2019 Jul 1;179:414-420.PMID:30999120DOI:10.1016/j.colsurfb.2019.03.039.
Liposomes are one of the most important and extensively studied drug delivery system due to their ability to encapsulate different kinds of drugs. Exploiting the advantages of 1H Nuclear Magnetic Resonance (NMR) spectrometry, we established a rapid and easy method for quantification of drugs encapsulated in liposomes. An internal standard, pyridine, was used for quantitative determination of drug concentration. Two different drugs were involved in this work, one hydrophilic, Methotrexate disodium salt, and another hydrophobic, tamoxifen. The specificity and selectivity of the suggested method were evaluated by the absence of overlapping of at least one signal of each drug with pyridine in the NMR spectrum. The accuracy and precision of the method were assessed by adding a known amount of each drug to unloaded liposomes. Results obtained by quantitative NMR (qNMR) were validated and confirmed by comparing with two other traditional techniques, Ultraviolet-Visible (UV-vis) spectrophotometry and High-Performance Liquid Chromatography (HPLC). It was found that the results were consistent with the ones obtained from our proposed qNMR method. Considering all the experiments conducted in this study, we deliberate that qNMR can be a suitable tool for the determination of drugs encapsulated in liposomes.
Design of biocompatible chitosan microgels for targeted pH-mediated intracellular release of cancer therapeutics
Biomacromolecules 2006 May;7(5):1568-72.PMID:16677040DOI:10.1021/bm050912z.
We report the rational design of a chitosan-based drug delivery system. The chitosan derivative N-[(2-hydroxy-3-trimethylammonium)propyl]chitosan chloride (HTCC) was ionically cross-linked by sodium tripolyphosphate (TPP) to form sub-200-nm microgels that are responsive to pH changes. When these microgels were loaded with Methotrexate disodium (MTX), a cytotoxic drug for cancer treatment, and conjugated to the targeting biomolecule apo-transferrin, a protein known to enter cells via receptor-mediated endocytosis, enhanced killing of immortalized HeLa cells was observed. In this intracellular delivery method, the microgel was exposed to low-pH environments that caused the chitosan to swell and release the drug. This rational drug delivery design may be useful in enhancing cancer therapy and reducing side effects.