Methotrexate

製品コードS1210 バッチS121006

印刷

化学情報

Synonyms

NCI-C04671, Amethopterin, CL14377, WR19039

Storage
(From the date of receipt)

3 years -20°C(in the dark) powder
1 year -80°C(in the dark) in solvent

化学式

C₂₀H₂₂N₈O₅

分子量

454.44

CAS No.

59-05-2

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

91 mg/mL (200.24 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	3.330mg/ml (7.33mM)	Taking the 1 mL working solution as an example, add 50 μL of 66.67 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Methotrexate, analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH. Methotrexate (MTX) induces apoptosis.
in vitro	Methotrexate (0.1-10 mM) induces apoptosis of in vitro activated T cells from human peripheral blood. This compound achieves clonal deletion of activated T cells in mixed lymphocyte reactions. It can selectively delete activated peripheral blood T cells by a CD95-independent pathway. ^[1] This chemical is taken up by cells via the reduced folate carrier and then is converted within the cells to polyglutamates. It leads to diminished production of leukotriene B4 by neutrophils stimulated ex vivo. Its polyglutamates inhibit the enzyme aminoimidazolecarboxamidoadenosineribonucleotide (AICAR) transformylase more potently than the other enzymes involved in purine biosynthesis. This compound 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. It suppresses the production of both TNF and IFN-γ by T-cell-receptor-primed T lymphocytes from both healthy human donors and RA patients. This 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]
in vivo	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. This compound-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]

製品説明

Methotrexate, analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH. Methotrexate (MTX) induces apoptosis.

in vitro

Methotrexate (0.1-10 mM) induces apoptosis of in vitro activated T cells from human peripheral blood. This compound achieves clonal deletion of activated T cells in mixed lymphocyte reactions. It can selectively delete activated peripheral blood T cells by a CD95-independent pathway. ^[1]

This chemical is taken up by cells via the reduced folate carrier and then is converted within the cells to polyglutamates. It leads to diminished production of leukotriene B4 by neutrophils stimulated ex vivo. Its polyglutamates inhibit the enzyme aminoimidazolecarboxamidoadenosineribonucleotide (AICAR) transformylase more potently than the other enzymes involved in purine biosynthesis. This compound 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. It suppresses the production of both TNF and IFN-γ by T-cell-receptor-primed T lymphocytes from both healthy human donors and RA patients. This 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]

in vivo

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. This compound-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]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Saos-2 cells
	濃度	0.1 μM
	反応時間	72 h
	実験の流れ	Cells were treated with indicated concentrations of this compound.
動物実験	動物モデル	Female Balb/c mice
	投薬量	0.05-0.5 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/9664073/
https://pubmed.ncbi.nlm.nih.gov/12106498/
https://pubmed.ncbi.nlm.nih.gov/8254024/

https://pubmed.ncbi.nlm.nih.gov/17696333/
https://pubmed.ncbi.nlm.nih.gov/35742867/

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カスタマーフィードバック

: , , ChemMedChem, 2015, 10(5):804-14.

: Data from [Data independently produced by , , Oncotarget, 2016, 7(17):23439-53]

: Data from [Data independently produced by , , J Cell Physiol, 2018, 233(5):3713-3722]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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Organoid drug profiling identifies methotrexate as a therapy for SCCOHT, a rare pediatric cancer [ Sci Adv, 2025, 11(9):eadq1724]	PubMed: 40009666
Identifying squalene epoxidase as a metabolic vulnerability in high-risk osteosarcoma using an artificial intelligence-derived prognostic index [ Clin Transl Med, 2024, 14(2):e1586]	PubMed: 38372422
NINJ1 regulates ferroptosis via xCT antiporter interaction and CoA modulation [ Cell Death Dis, 2024, 15(10):755]	PubMed: 39424803
EFNB1 levels determine distinct drug response patterns guiding precision therapy for B-cell neoplasms [ iScience, 2024, 27(1):108667]	PubMed: 38155773
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862]	PubMed: 39319271
Studying Target-Engagement of Anti-Infectives by Solvent-Induced Protein Precipitation and Quantitative Mass Spectrometry [ ACS Infect Dis, 2024, 10(12):4087-4102]	PubMed: 39566904
Wogonin inhibits the migration and invasion of fibroblast-like synoviocytes by targeting PI3K/AKT/NF-κB pathway in rheumatoid arthritis [ Arch Biochem Biophys, 2024, 755:109965]	PubMed: 38552763

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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