Methotrexate

製品コードS1210 バッチS121006

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	91 mg/mL warmed with 50ºC water bath (200.24 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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. 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]
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. 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]

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. 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]

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. 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]

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 drug.
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

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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：

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
EFNB1 levels determine distinct drug response patterns guiding precision therapy for B-cell neoplasms [ iScience, 2024, 27(1):108667]	PubMed: 38155773
NINJ1 regulates ferroptosis via xCT antiporter interaction and CoA modulation [ bioRxiv, 2024, 2024.02.22.581432]	PubMed: 38464226
Patient- and xenograft-derived organoids recapitulate pediatric brain tumor features and patient treatments [ EMBO Mol Med, 2023, 15(12):e18199]	PubMed: 38037472
USP11-mediated LSH deubiquitination inhibits ferroptosis in colorectal cancer through epigenetic activation of CYP24A1 [ Cell Death Dis, 2023, 14(7):402]	PubMed: 37414755
A novel antifolate suppresses growth of FPGS-deficient cells and overcomes methotrexate resistance [ Life Sci Alliance, 2023, 6(11)e202302058]	PubMed: 37591722
miR-197-3p Promotes Osteosarcoma Stemness and Chemoresistance by Inhibiting SPOPL [ J Clin Med, 2023, 12(3)1177]	PubMed: 36769824
Modeling drug-induced liver injury and screening for anti-hepatofibrotic compounds using human PSC-derived organoids [ Cell Regen, 2023, 12(1):6]	PubMed: 36864321
A pH-Responsive DNA Tetrahedron/Methotrexate Drug Delivery System Used for Rheumatoid Arthritis Treatment [ J Funct Biomater, 2023, 10.3390/jfb14110541]	PubMed: 37998110
Multi-omics analysis based on 3D-bioprinted models innovates therapeutic target discovery of osteosarcoma [ Bioact Mater, 2022, 18:459-470]	PubMed: 35415297

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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