A7019
(+)-氨甲蝶呤 水合物
≥95%, powder
别名:
MTX, 氨甲叶酸, 氨甲喋呤
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关于此项目
经验公式（希尔记法）:
C20H22N8O5 · xH2O
化学文摘社编号:
分子量:
454.44 (anhydrous basis)
UNSPSC Code:
12352200
PubChem Substance ID:
EC Number:
262-213-7
MDL number:
SMILES string
O.CN(Cc1cnc2nc(N)nc(N)c2n1)c3ccc(cc3)C(=O)NC(CCC(O)=O)C(O)=O
assay
≥95%
form
powder
color
yellow to yellow with an orange cast
solubility
H2O: insoluble
storage temp.
−20°C
Gene Information
human ... DHFRP1(573971), FPGS(2356), SLC19A1(6573), TYMS(7298)
mouse ... Dhfr(13361)
rat ... Dhfr(24312)
Application
Amethopterin is a folic acid antagonist and potent anticancer agent. Amethopterin blocks DNA synthesis by preventing the production of tetrahydrofolate cofactors which are required to make thymidine. Amethopterin is actively transported into cells by the folate transporter where it is converted to a high molecular weight polyglutamate metabolite by folylpolyglutamate synthase, a dihydrofolate reductase inhibitor.
Biochem/physiol Actions
Amethopterin is a folic acid antagonist and potent anticancer agent. Blocks DNA synthesis by blocking the production of tetrahydrofolate covactors required for the synthesis of thymidine. Amethopterin is actively transported into cells by the folate transporter. In the cell, it is converted to a high molecular weight polyglutamate metabolite by folylpolyglutamate synthase that, in turn, binds to dihydrofolate reductase and inhibits its activity. Amethopterin-polyglutamate is degraded intracellularly by γ-glutamyl hydrolase.
Preparation Note
Add a minimal amount of 0.1 N NaOH to solubilize, then dilute in neutral buffer or saline. Diluted stock is stable for 1 week refrigerated and for 1 month frozen at −20 °C. References: Cell & Tissue Culture: Laboratory Procedures, Chapter 27, Page 27D:3.2 (A. Doyle, et al., eds, John Wiley) and Cell Biology: A Laboratory Handbook, vol. 2, page 417 (Julio E. Celis, ed., Academic Press).
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Oral - Eye Irrit. 2 - Repr. 1B - Skin Irrit. 2
存储类别
6.1B - Non-combustible acute toxic Cat. 1 and 2 / very toxic hazardous materials
wgk
WGK 3
ppe
Eyeshields, Faceshields, Gloves, type P3 (EN 143) respirator cartridges
法规信息
新产品
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Roy Fleischmann et al.
Annals of the rheumatic diseases, 74(6), 1132-1137 (2014-08-22)
Disease Activity Score in 28 joints calculated with C-reactive protein (DAS28-CRP) is used instead of erythrocyte sedimentation rate (DAS28-ESR) to assess rheumatoid arthritis disease activity; however, values for remission and low disease activity (LDA) for DAS28-CRP have not been validated.
Christian S Kaas et al.
Biotechnology journal, 10(7), 1081-1089 (2015-05-13)
Coagulation factor VIII (FVIII) is one of the most complex biopharmaceuticals due to the large size, poor protein stability and extensive post-translational modifications. As a consequence, efficient production of FVIII in mammalian cells poses a major challenge, with typical yields
Joshua F Baker et al.
Annals of the rheumatic diseases, 73(11), 1968-1974 (2013-08-02)
To determine if early MRI measures predict X-ray progression at 1 and 2 years in a large RA trial cohort. This study included 256 methotrexate (MTX)-naïve RA patients from a randomised placebo-controlled trial of golimumab (GO-BEFORE). MRIs of wrist and 2nd-5th
Kalle Jyri Aaltonen et al.
The Journal of rheumatology, 42(3), 372-378 (2015-01-17)
Because of the role of tumor necrosis factor (TNF) in host defense, it was hypothesized that its inhibition might lead to an increased risk of malignancies and infections. The objective of our study was to assess the incidence of serious
Axel Finckh et al.
Arthritis research & therapy, 16(5), 458-458 (2014-10-16)
Calcium pyrophosphate deposition (CPPD) may cause severe arthropathy, major joint destruction and treatment options are limited. The aim of this study was to test the therapeutic efficacy of methotrexate (MTX) in chronic or recurrent CPPD arthropathy. Patients with CPPD arthropathy
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