CAS No. : 59-05-2

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For research use only. Not Intended for Therapeutic Use!
Cat No:I000021
Synonyms:(2S)-2-[[4-[(2,4-diaminopteridin-6-yl)methyl-methylamino]benzoyl]amino]pentanedioic acid
Molecular Formula:C20H22N8O5
Molecular Weight:454.4
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Appearance:A crystalline solid
Cat No:I000021
Cas No:59-05-2

Methotrexate(WR19039; CL14377) can interfere with the growth of certain cells of the body, especially cells that reproduce quickly, such as cancer cells, bone marrow cells, and skin cells.
IC50 Value:
Target: antifolate
in vitro: In normal T cells, Methotrexate (MTX) produced a dose-dependent reduction in de novo adenosine and guanosine pools with maximal effects (>50%) at 1 microM MTX. In CEM cells, de novo purine synthesis was almost completely blocked by 1 microM MTX. Total purine pools were also reduced in both cell types after MTX treatment [1]. JAR cells underwent apoptosis after exposure to 0.1-2.5 microg/ml MTX for 48 h. Decreased mitochondrial membrane potential was observed both by fluorescence microscopy and FCM. The activation of caspase-9 was increased 4.35+/-0.76-fold in MTX-incubated JAR, while there was no obvious change in the activation of caspase-8 [2].
in vivo: Three, four and five weeks after consecutive administration of MTX (3 mg/kg/day), hydroxyproline content in the lung tissues increased significantly to about 2 times higher that of the control level [3]. MTX was administered intraperitoneally (ip) at the doses of 5, 10, 20 and 40 mg/kg to mice (20-25 g) weekly once (wk) for 5 and 10 weeks. The animals were sacrificed 1 week after receiving the last treatment of MTX. The germ cell toxicity was evaluated using testes weight (wt), sperm count, sperm head morphology, sperm comet assay, histology, TUNEL and halo assay in testis. MTX treatment significantly reduced the sperm count and increased the occurrence of sperm head abnormalities in a dose dependent manner [4].
Toxicity: MTX could induce alveolar epithelial cell injury and resulted in the loss of integrity of the alveolar-capillary barrier basement membranes followed by the recruitment and proliferation of myofibroblasts with the deposition of collagens [3]. A total of 94 different side effects were reported. The most commonly reported problem was alopecia (mean incidence = 91%), followed by fatigue (89%), and weight gain (68%) [5].

1:Polymorphisms in methotrexate transporters and their relationship to plasma methotrexate levels, toxicity of high-dose methotrexate, and outcome of pediatric acute lymphoblastic leukemia. Liu SG, Gao C, Zhang RD, Zhao XX, Cui L, Li WJ, Chen ZP, Yue ZX, Zhang YY, Wu MY, Wang JX, Li ZG, Zheng HY.Oncotarget. 2017 May 10. doi: 10.18632/oncotarget.17781. [Epub ahead of print] PMID: 28525903
2:Cost-utility analysis of certolizumab pegol in combination with methotrexate in patients with moderate-to-severe active rheumatoid arthritis in Greece. Tzanetakos C, Tzioufas A, Goules A, Kourlaba G, Theodoratou T, Christou P, Maniadakis N.Rheumatol Int. 2017 May 18. doi: 10.1007/s00296-017-3736-z. [Epub ahead of print] PMID: 28523420
3:Methotrexate encephalopathy: Two cases in adult cancer patients, who recovered with pathophysiologically based therapy. Coker SA, Pastel DA, Davis MC, Bengtson EM, Fadul CE, Lewis LD.SAGE Open Med Case Rep. 2017 May 4;5:2050313X17706875. doi: 10.1177/2050313X17706875. eCollection 2017. PMID: 28515935
4:HLA-Cw6-positive patients with psoriasis show improved response to methotrexate treatment. West J, Ogston S, Berg J, Palmer C, Fleming C, Kumar V, Foerster J.Clin Exp Dermatol. 2017 May 17. doi: 10.1111/ced.13100. [Epub ahead of print] PMID: 28512993
5:Histopathological Features of Methotrexate Induced Pulmonary Lesions in Rheumatoid Arthritis Patients: A Systematic Review of Case Reports. Thaniyan A, Ayman FFA, Mirghani HO, Al-Sayed BA, Merghani TH.Open Access Maced J Med Sci. 2017 Apr 8;5(2):266-270. doi: 10.3889/oamjms.2017.049. eCollection 2017 Apr 15. Review. PMID: 28507640 Free PMC Article
6:Methotrexate: an effective monotherapy for refractory generalized morphea. Platsidaki E, Tzanetakou V, Kouris A, Stavropoulos PG.Clin Cosmet Investig Dermatol. 2017 May 8;10:165-169. doi: 10.2147/CCID.S134879. eCollection 2017. PMID: 28507446 Free PMC Article
7:Quantitative on-line liquid chromatography-surface- enhanced Raman scattering (LC-SERS) of methotrexate and its major metabolites. Subaihi A, Trivedi DK, Hollywood KA, Bluett J, Xu Y, Muhamadali H, Ellis DI, Goodacre R.Anal Chem. 2017 May 15. doi: 10.1021/acs.analchem.7b00916. [Epub ahead of print] PMID: 28505414
8:Mizoribine Synchronized Methotrexate Therapy should be Considered when Treating Rheumatoid Arthritis Patients with an Inadequate Response to Various Combination Therapies. Ikeda K, Watanabe K, Hirai T, Tanji K, Miyashita T, Nakajima S, Uomori K, Morimoto S, Takamori K, Ogawa H, Takasaki Y, Sekigawa I.Intern Med. 2017;56(10):1147-1152. doi: 10.2169/internalmedicine.56.7886. Epub 2017 May 15. PMID: 28502927 Free Article
9:Nausea and vomiting in children and adolescents receiving intrathecal methotrexate: A prospective, observational study. Flank J, Nadeem K, Moledina S, Khanna M, Schindera C, Punnett A, Dupuis LL.Pediatr Blood Cancer. 2017 May 13. doi: 10.1002/pbc.26603. [Epub ahead of print] PMID: 28500750
10:Response to: /'HLA-A* 31:01 is not associated with the development of methotrexate pneumonitis in the UK population: results from a genome wide association study/' by Bluett et al. Furukawa H, Oka S, Shimada K, Tsuchiya N, Tohma S; Rheumatoid Arthritis associated Interstitial Lung Disease (RA-ILD) Study Consortium..Ann Rheum Dis. 2017 May 12. pii: annrheumdis-2017-211518. doi: 10.1136/annrheumdis-2017-211518. [Epub ahead of print] No abstract available. PMID: 28500058
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