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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBusulfanCat. No.: HY-B0245CAS No.: 55-98-1分式: CHOS分量: 246.3作靶點: DNA Alkylator/Crosslinker作通路: Cell Cycle/DNA Damage儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 30 mg/mL (121.80 mM)* mean
2、s soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 4.0601 mL 20.3004 mL 40.6009 mL5 mM 0.8120 mL 4.0601 mL 8.1202 mL10 mM 0.4060 mL 2.0300 mL 4.0601 mL請根據(jù)產品在不同溶劑中的溶解度,選擇合適的溶劑配制儲備液,并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Busulfan種有效的烷化劑,對髓具有選擇性免疫抑制作。IC50 & Target DNA A
3、lkylator 1體外研究Busulfan is a potent alkylating agent, and used as a chemotherapeutic agent. Busulfan (120 M) results inpremature senescence in WI38 cells via the Erk and p38 MAPK pathway, reduces GSH and increases ROS1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEproduction, but the production can
4、be suppressed by NADPH oxidase 1.體內研究 Busulfan (40 mg/kg, i.p) increases apoptosis and decreases the testis weight in mice. The testes of Busulfan-treated mice exhibits higher level of pRB expression, inhibits Rb phosphorylation and PCNA expressioncompared to the control 2. Busulfan (2.5, 5.0 mg/kg,
5、 i.p.) causes earlier occurrence of persistent esturs in adose dependent manner in rats. Busulfan (5.0 mg/kg) also increases the incidence of uterineadenocarcinomas and multiplicity of uterine neoplastic lesions. In addition, Busulfan decreases the serum 17-estradiol(E2), progesterone and inhibin le
6、vels in rats, and elevates the E2/progesterone ratio only at 5.0mg/kg 3.PROTOCOLCell Assay 1 WI38 cells are seeded in wells of a 24-well plate at 60,000 cells/well and cultured overnight. They are treatedwith Busulfan for 24 h, after which the drug is removed and the cells are cultured in fresh medi
7、um for up to 11d. Untreated cells are used as control. Every 3 d the cells are trypsinized, counted and sub-cultured in a freshmedium at 1:5 and 1:2 dilutions for control untreated and Busulfan-treated cells, respectively 1.MCE has not independently confirmed the accuracy of these methods. They are
8、for reference only.Animal Mice 2Administration 2 One hundred twenty ICR male mice ranging in age from 8 to 12 weeks (30-40 g) are used. Eight-week-oldICR male mice receive a single intraperitoneal injection of Busulfan (40 mg/kg) diluted in sesame oil. Themice are housed in wire cages at 22 1C under
9、 a 12-h light-dark cycle with 70% humidity and fed ad libitum2.MCE has not independently confirmed the accuracy of these methods. They are for reference only. J Mol Med (Berl). 2019 Jun 14. Stem Cells Dev. 2019 Jul 16. Asian J Androl. 2019 Jun 7.See more customer validations on HYPERLINK / www.MedCh
10、emEREFERENCES1. Probin V, et al. Busulfan-induced senescence is dependent on ROS production upstream of the MAPK pathway. Free Radic Biol Med.2007 Jun 15;42(12):1858-65. Epub 2007 Mar 31.2. Choi YJ, et al. Murine male germ cell apoptosis induced by busulfan treatment correlates with loss of c-kit-ex
11、pression in a Fas/FasL- andp53-independent manner. FEBS Lett. 2004 Sep 24;575(1-3):41-51.3. Yoshida M, et al. Reduction of primordial follicles caused by maternal treatment with busulfan promotes endometrial adenocarcinomadevelopment in donryu rats. J Reprod Dev. 2005 Dec;51(6):707-14. Epub 2005 Sep 22.McePdfHeight2/2 Master of Small Molecules 您邊的抑制劑師www.MedChemECaution: Product has n
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