6-Mercaptopurine hydrate

An inhibitor of purine synthesis and interconversion

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50mg

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货号: ajce50192
CAS: 6112-76-1
别名: 6-巯基嘌呤一水合物; Mercaptopurine hydrate; 6-MP hydrate
分子式: C5H6N4OS
分子量: 170.19
纯度: >98%
溶解度: DMSO : 32 mg/mL (188.03 mM)
储存: Store at -20°C
库存: 现货

Background

6-Mercaptopurine (6-MP) is an inhibitor of purine synthesis and interconversion.¹ It is rapidly converted to 6-mercaptopurine ribonucleoside-5'-monophosphate, which inhibits phosphoribosyl pyrophosphate (PRPP) amidotransferase, the rate-limiting enzyme in purine synthesis. It also inhibits the conversion of IMP to adenylosuccinic acid and xanthylic acid and blocks AMP formation in vitro. 6-MP (30 mg/kg) inhibits growth of sarcoma 180, adenocarcinoma E 0771, and adenocarcinoma 755 tumors and reduces the size of leukemia L1210 subcutaneous growths in mice.² It also decreases delayed-type hypersensitivity and thyroid inflammation in a guinea pig model of thyroiditis when administered pre- or post-disease onset.³ Formulations containing mercaptopurine have been used for maintenance therapy in patients with acute lymphoblastic leukemia.⁴

1.Brockman, R.W.Biochemical aspects of mercaptopurine inhibition and resistanceCancer Res.23(8)1191-1201(1963) 2.Skipper, H.E., Thomson, J.R., Elion, G.B., et al.Observations on the anticancer activity of 6-mercaptopurineCancer Res.14(4)294-298(1954) 3.Spiegelberg, H.L., and Miescher, P.A.The effect of 6-mercaptopurine and aminopterin on experimental immune thyroiditis in guinea pigsJ. Exp. Med.118(5)869-890(1963) 4.Alsous, M., Abu Farha, R., Alefishat, E., et al.Adherence to 6-mercaptopurine in children and adolescents with acute lymphoblastic leukemiaPLoS One12(9)e0183119(2017)

Protocol

Kinase experiment:	L6 myotubes are treated with DMSO control or 6-Mercaptopurine hydrate (6-MP) for 24 h, with the final 3 h of incubation including treatments in serum-free DMEM, and further incubated in the absence or presence of 100 nM insulin for 60 min at 37°C. Then, protein lysates (50 μg) are collected and subjected to SDS-PAGE. The proteins are finally quantified by densitometric analysis of scanned films using Image J software[2].
Cell experiment:	Cell viability is measured using Cell Viability Assay. L6 skeletal muscle cells are seeded in 96-well plates at a density of 10,000 cells/well and differentiated into myotubes within 7 days. Cells are treated with different doses of 6-Mercaptopurine hydrate (6-MP) for 24 h before the assay. For analysis of cell viability, plates are equilibrated at room temperature for 30 min; 50 μL of Cell Titer-Glo reagent is added to each well, and plates are mixed for 12 min on an orbital shaker. Luminescence is quantified using a luminometer[2].
Animal experiment:	Around thirteen-week-old pregnant rats are used in this study. The animals are housed individually in wire-mesh cages in an air-conditioned room (temperature, 23±3°C; humidity, 50±20%; ventilation, 10 times/hour; lighting, 12 h light to12 h dark cycle) and are given pelleted diet and water ad libitum. In the experiment, fifteen pregnant rats are injected i.p. with 50 mg/kg 6-Mercaptopurine hydrate (6-MP) on E13, and three dams each are sacrificed by exsanguination from the abdominal aorta under ether anesthesia at 12, 24, 36, 48, and 72 h. Fetuses are collected from each dam by Caesarean section. As controls, fifteen pregnant rats are injected i.p. with 2.0% methylcellulose solution in distilled water at E13, and three dams are sacrificed at each of the same time-points[3].
参考文献: [1]. Sahasranaman S, et al. Clinical pharmacology and pharmacogenetics of thiopurines. Eur J Clin Pharmacol. 2008 Aug;64(8):753-67. [2]. Liu Q, et al. 6-Mercaptopurine augments glucose transport activity in skeletal muscle cells in part via a mechanism dependent upon orphan nuclear receptor NR4A3. Am J Physiol Endocrinol Metab. 2013 Nov 1;305(9):E1081-92. [3]. Kanemitsu H, et al. 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.