白消安作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetBusulfanCat. No.: HY-B0245CAS No.: 55-98-1分式: CHOS分量: 246.3作靶點(diǎn): DNA Alkylator/Crosslinker; Apoptosis作通路: Cell Cycle/DNA Damage; Apoptosis儲(chǔ)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(shí)驗(yàn) DMSO : 50 mg/mL (203.00 mM; Need ultrasonic)H2O : 0.1 mg/mL (inso

2、luble)SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)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(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和

3、給藥式選擇適當(dāng)?shù)娜芙獍浮Ｒ韵氯芙獍付颊埾劝凑?In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (10.15 mM); Clear solution此案可獲得 2.5 mg/mL (10.15 mM，飽和度未知) 的

4、澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (10.15 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (10.15 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25

5、.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (10.15 mM); Clear solution此案可獲得 2.5 mg/mL (10.15 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Busulfan種有效的烷化劑，對髓具有選擇性免

6、疫抑制作。IC & Target DNA Alkylator1體外研究 Busulfan is a potent alkylating agent, and used as a chemotherapeutic agent. Busulfan (120 M) results in prematuresenescence in WI38 cells via the Erk and p38 MAPK pathway, reduces GSH and increases ROS production, but theproduction can be suppressed by NADPH oxid

7、ase1.體內(nèi)研究 Busulfan (40 mg/kg, i.p) increases apoptosis and decreases the testis weight in mice. The testes of Busulfan-treatedmice exhibits higher level of pRB expression, inhibits Rb phosphorylation and PCNA expression compared to the control2. Busulfan (2.5, 5.0 mg/kg, i.p.) causes earlier occurre

8、nce of persistent esturs in a dose dependent manner inrats. Busulfan (5.0 mg/kg) also increases the incidence of uterine adenocarcinomas and multiplicity of uterineneoplastic lesions. In addition, Busulfan decreases the serum 17-estradiol(E2), progesterone and inhibin levels in rats,and elevates the

9、 E2/progesterone ratio only at 5.0 mg/kg3.PROTOCOLCell Assay 1 WI38 cells are seeded in wells of a 24-well plate at 60,000 cells/well and cultured overnight. They are treated withBusulfan for 24 h, after which the drug is removed and the cells are cultured in fresh medium for up to 11 d.Untreated ce

10、lls are used as control. Every 3 d the cells are trypsinized, counted and sub-cultured in a fresh medium at1:5 and 1:2 dilutions for control untreated and Busulfan-treated cells, respectively1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice2

11、Administration 2 One hundred twenty ICR male mice ranging in age from 8 to 12 weeks (30-40 g) are used. Eight-week-old ICR malemice receive a single intraperitoneal injection of Busulfan (40 mg/kg) diluted in sesame oil. The mice are housed inwire cages at 22 1C under a 12-h light-dark cycle with 70

12、% humidity and fed ad libitum2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Mol Med (Berl). 2019 Aug;97(8):1183-1193. Exp Cell Res. 2020 May 3:112054. Stem Cells Dev. 2020 Feb 5.Page 2 of 3 www.MedChemE Stem Cells Dev. 2019 Jul 16. Asia

13、n J Androl. 2019 Jun 7.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Probin V, et al. Busulfan-induced senescence is dependent on ROS production upstream of the MAPK pathway. Free Radic Biol Med. 2007 Jun15;42(12):1858-65. Epub 2007 Mar 31.2. Choi YJ, et al. Murine

14、 male germ cell apoptosis induced by busulfan treatment correlates with loss of c-kit-expression in a Fas/FasL- and p53-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 adenocarcinoma development indonryu rats. J Reprod Dev. 2005 Dec;51(6):707-14. Epub 2005 Sep 22.McePdfH