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6-Mercaptopurine hydrate

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Chemical Structure| 6112-76-1 同义名 : 6-巯基嘌呤一水合物 ;6-Mercaptopurine monohydrate;Mercaptopurine hydrate;6-MP;6-Mercaptopurine (hydrate);6-MP hydrate
CAS号 : 6112-76-1
货号 : A189537
分子式 : C5H6N4OS
纯度 : 98%
分子量 : 170.192
MDL号 : MFCD03854445
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(293.79 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 6-Mercaptopurine Monohydrate is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive drug. 6-MP induced G2/M arrest, delayed S-phase progression, and finally induced apoptosis of neural progenitor cells mediated by p53 in the fetal rat telencephalon[3]. The thiopurine drugs azathioprine and 6-mercaptopurine (6-MP) are well-established in the treatment of inflammatory bowel disease (IBD) [4]. The mode of action of azathioprine is thought to be multifactorial, including conversion to 6-mercaptopurine (which acts as a purine antimetabolite), possible blockade of thiol groups by alkylation, inhibition of several pathways in nucleic acid biosynthesis (preventing proliferation of cells involved in the determination and amplification of the immune response) and damage to DNA through the incorporation of thiopurine analogues. Azathioprine and 6-mercaptopurine are further known to alter lymphocyte function, reduce the number of lamina propria plasma cells and affect natural killer cell function[5]. 6-Mercaptopurine monohydrate (6-MP) was administered intraperitoneally (i.p.) or orally (p.o.) to 2 strains of mice, MS/Ae and CD-1. From the results of an acute toxicity test and a pilot micronucleus test, the doses selected for the final micronucleus test were 12.5-100 mg/kg for the i.p. route and 25-200 mg/kg for the p.o. route[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00819351 Acute Lymphoblastic Leukemia Phase 3 Completed - Denmark ... 展开 >> Department of Pediatrics, Rigshospitalet Copenhagen, Denmark, 2100 Finland Helsinki University Hospital Helsinki, Finland Iceland University Hospital Reykjavik, Iceland Reykjavik, Iceland Norway Trondheim University Hospital Trondheim, Norway Sweden Department of Pediatrics, Drottning Sylvias Pediatric Hospital Gothenburg, Sweden NOPHO nordic organisation for pediatric onology Stockholm, Sweden 收起 <<
NCT00609973 - Completed - -
NCT01458951 Ulcerative Colitis Phase 3 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.88mL

1.18mL

0.59mL

29.38mL

5.88mL

2.94mL

58.76mL

11.75mL

5.88mL
参考文献

[1]Sahasranaman S, Howard D, Roy S. Clinical pharmacology and pharmacogenetics of thiopurines. Eur J Clin Pharmacol. 2008 Aug;64(8):753-67.

[2]Weinshilboum RM, Sladek SL. Mercaptopurine pharmacogenetics: monogenic inheritance of erythrocyte thiopurine methyltransferase activity. Am J Hum Genet. 1980 Sep;32(5):651-62.

[3]Kanemitsu H, Yamauchi H, Komatsu M, Yamamoto S, Okazaki S, Uchida K, Nakayama H. 6-Mercaptopurine (6-MP) induces cell cycle arrest and apoptosis of neural progenitor cells in the developing fetal rat brain. Neurotoxicol Teratol. 2009 Mar-Apr;31(2):104-9

[4]Gearry RB, Barclay ML. Azathioprine and 6-mercaptopurine pharmacogenetics and metabolite monitoring in inflammatory bowel disease. J Gastroenterol Hepatol. 2005 Aug;20(8):1149-57

[5]Nielsen OH, Vainer B, Rask-Madsen J. Review article: the treatment of inflammatory bowel disease with 6-mercaptopurine or azathioprine. Aliment Pharmacol Ther. 2001 Nov;15(11):1699-708

[6]Hara T, Makita T, Horiya N, Ozawa S, Ohba M, Naito J, Shibuya T. Micronucleus test with 6-mercaptopurine monohydrate administered intraperitoneally and orally. Mutat Res. 1989 Aug;223(4):349-52