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6-巯基嘌呤一水合物 /6-Mercaptopurine hydrate {[allProObj[0].p_purity_real_show]}

货号:A189537 同义名: 6-巯基嘌呤一水合物 / 6-Mercaptopurine monohydrate;Mercaptopurine hydrate

6-Mercaptopurine Monohydrate inhibits the de novo purine synthesis through incorporation of thiopurine methyltransferase metabolites into DNA and RNA, it is a widely used antileukemic agent and immunosuppressive drug. 6-mercaptopurine was found to inhibit SARS-CoV PLpro.

6-Mercaptopurine hydrate 化学结构 CAS号:6112-76-1
6-Mercaptopurine hydrate 化学结构
CAS号:6112-76-1
6-Mercaptopurine hydrate 3D分子结构
CAS号:6112-76-1
6-Mercaptopurine hydrate 化学结构 CAS号:6112-76-1
6-Mercaptopurine hydrate 3D分子结构 CAS号:6112-76-1
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6-Mercaptopurine hydrate 纯度/质量文件 产品仅供科研

货号:A189537 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 DNA synthesis helicase RdRp ribonucleotide reductase tRNA synthetase YB-1 其他靶点 纯度
Fexinidazole 98%
Daptomycin 98%
Blasticidin S·HCl 98%
Metronidazole 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

98%
Triglycidyl isocyanurate p53 98+%
Nedaplatin 99%+
Bendamustine 98+%
Trifluridine 98%
Robinetin 99%+
Carboplatin 99%
Cidofovir 99%
Cisplatin 99%
Cytarabine ++++

DNA synthesis, IC50: 16 nM

98%
Acelarin ++++

DNA synthesis, EC50: 0.2 nM

99%+
Oxaliplatin 98%
YK-4-279 99%+
ML216 +

BLMfull-length, IC50: 2.98 μM

BLM636-1298, IC50: 0.97 μM

99%+
RK-33 98%
Brr2-IN-3 99%+
Phen-DC3 Trifluoromethanesulfonate 98%
Favipiravir 97%
Suramin sodium salt ++

RdRp, IC50: 0.26 μM

99%+
Clofarabine ++

Ribonucleotide reductase, IC50: 65 nM

97%
Didox 98%
(E)-3-AP 97%
Halofuginone +++

prolyl-tRNA synthetase, Ki: 18.3nM

99%+
BC-LI-0186 +++

Leucyl-tRNA synthetase, Kd: 42.1 nM

Leucyl-tRNA synthetase, IC50: 46.11 nM

98%
SU056 +

YB-1, IC50: 1.73 μM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

6-Mercaptopurine hydrate 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].

6-Mercaptopurine hydrate 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 - -

6-Mercaptopurine hydrate 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

6-Mercaptopurine hydrate 实验方案

计算器
存储液制备 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

6-Mercaptopurine hydrate 技术信息

CAS号6112-76-1
分子式C5H6N4OS
分子量 170.192
别名 6-巯基嘌呤一水合物 ;6-Mercaptopurine monohydrate;Mercaptopurine hydrate;6-MP;6-Mercaptopurine (hydrate);6-MP hydrate
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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
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