Methotrexate
Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia) [1][2][3].
Product Specifications
CAS Number
[59-05-2]
Product Name Alternative
Amethopterin; CL14377; WR19039
UNSPSC
12352203
Hazard Statement
H301, H315, H319, H341, H360
Target
ADC Payload; Antifolate; Apoptosis; Bacterial; DNA/RNA Synthesis
Type
ADC Related
Related Pathways
Antibody-drug Conjugate/ADC Related; Anti-infection; Apoptosis; Cell Cycle/DNA Damage
Applications
Cancer-programmed cell death
Field of Research
Cancer; Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/Methotrexate.html
Concentration
10mM
Purity
99.87
Solubility
DMSO : ≥ 50 mg/mL
Smiles
NC1=NC(N)=C2C(N=CC(CN(C)C3=CC=C(C(N[C@@H](CCC(O)=O)C(O)=O)=O)C=C3)=N2)=N1
Molecular Formula
C20H22N8O5
Molecular Weight
454.44
Precautions
H301, H315, H319, H341, H360
References & Citations
[1]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 in Rat Large Intestine.|[4]Banji D, et al. Evaluation of the concomitant use of methotrexate and curcumin on Freund's complete adjuvant-induced arthritis and hematological indices in rats. Indian J Pharmacol. 2011;43 (5) :546-550.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, protect from light)
Scientific Category
ADC Related
Clinical Information
Launched
Isoform
Traditional Cytotoxic Agents
Citation 01
ACS Omega. 2025 Oct 29;10 (44) :52562–52575.|Acta Biomater. 2025 Aug 27:S1742-7061 (25) 00640-3.|Acta Pharmacol Sin. 2021 Jan;42 (1) :108-114.|Acta Pharmacol Sin. 2025 Jun;46 (6) :1733-1741.|Adv Mater. 2025 Jul 4:e2505231.|Anticancer Res. 2024 Jul;44 (7) :2787-2792.|Anticancer Res. 2024 Oct;44 (10) :4213-4218.|Arthritis Res Ther. 2022 Jan 19;24 (1) :27.|Authorea. 2025 Jan 03.|Biochem Biophys Rep. 2021 Nov 26:28:101177.|Biomed Pharmacother. 2024 Jul 19:178:117167.|bioRxiv. 2025 Nov 20.|Biotechnol Bioeng. 2021 Dec;118 (12) :4687-4698.|Cancers (Basel) . 2022 Oct 19;14 (20) :5127.|Cancers. 2019 Oct 25;11 (11) :1654.|Cell Death Dis. 2020 Nov 12;11 (11) :976.|Cell Death Dis. 2024 May 20;15 (5) :349.|Cell Death Dis. 2025 Nov 24;16 (1) :852.|Cell Death Dis. 2025 Nov 24;16 (1) :856.|Cell Rep Med. 2025 Apr 2:102053.|Cell Rep Methods. 2023 Oct 23;3 (10) :100599.|Chem Res Toxicol. 2025 Feb 17;38 (2) :281-295.|Commun Biol. 2022 Jun 23;5 (1) :619.|Dis Model Mech. 2023 Mar 1;16 (3) :dmm049769.|Ecotoxicol Environ Saf. 2025 Nov 15:307:119433.|EMBO Mol Med. 2022 Mar 7;14 (3) :e14552.|EMBO Mol Med. 2025 Oct 13.|Eur J Pharm Sci. 2025 Sep 27:214:107296.|Eur J Pharmacol. 2023 Dec 15:961:176162.|Guidelines and Standards in Chinese Medicine. 2024 Dec.|Int Immunopharmacol. 2023 Feb:115:109689.|Int Immunopharmacol. 2023 Nov 15;125 (Pt B) :111175.|Int Immunopharmacol. 2024 Jun 15:134:112183.|Int Immunopharmacol. 2025 Apr 26:156:114735.|Int Immunopharmacol. 2025 May 23:159:114894.|Int J Immunopathol Pharmacol. 2025 Jan-Dec:39:3946320251348715.|J Adv Res. 2025 Aug:74:609-620.|J Biol Chem. 2019 Dec 27;294 (52) :20084-20096. |J Bone Oncol. 2021 Sep 20:30:100391.|J Clin Invest. 2023 Jul 3;133 (13) :e169993.|J Exp Clin Cancer Res. 2024 Dec 26;43 (1) :330.|J Mol Med (Berl) . 2019 Aug;97 (8) :1183-1193.|J Nanobiotechnology. 2024 Mar 3;22 (1) :89.|J Pharm Anal. 2022 Dec;12 (6) :879-888.|Lung. 2024 Nov 27;203 (1) :4.|Mediators Inflamm. 2024 Dec 5:2024:1995952.|Micromachines. 2021 Jun 10;12 (6) :681.|Mol Biomed. 2025 Nov 21;6 (1) :114.|Mol Cancer. 2024 Apr 29;23 (1) :86.|Mol Cancer. 2024 Jan 10;23 (1) :12.|Nat Commun. 2025 Feb 28;16 (1) :2071.|Oncotarget. 2017 Dec 2;8 (68) :112313-112329.|Patent. US20170128439A1.|Patent. US20250235423A1.|Phytomedicine. 2022 Jun;100:154068.|Plasma Process Polym. 2021 Feb 12.|Queen’s University. Department of Biomedical Molecular Sciences. 2021 Oct.|Redox Biol. 2024 Dec 25:79:103482.|Research Square Preprint. 2023 Dec 1.|Research Square Preprint. 2023 Dec 4.|Rheumatology (Oxford) . 2025 Aug 13:keaf437.|Sci Rep. 2018 Jun 21;8 (1) :9472. |Sci Rep. 2024 Oct 31;14 (1) :26224.|Sci Signal. 2024 Nov 26;17 (864) :eadp1375.|Small. 2022 Jul;18 (30) :e2202337.|SSRN. 2025 Oct 10.|Toxicology. 2020 May 15;437:152445.|Biomater Res. 2025 Sep 3:29:0245.|Cell Rep. 2025 Mar 25;44 (4) :115466.|Mol Immunol. 2025 Apr 16:182:83-95.|Sci Data. 2024 Sep 19;11 (1) :1024.
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