产品说明书
Busulfan
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同义名 : | 1,4-双甲基硫氧基丁烷 ;Busulphan;NSC-750;14di(methylsulfonyloxy)butane.;14di(methanesulfonyloxy)butane;14butanediol dimethylsulfonate;14bitanediol dimethanesulfonate esters;14bis(methanesulfonoxy)butane;Chemical structure names: ;WR19508;GT41;Code names: CB2041;BUS;Abbreviations: BU;Misulfan;Misulban;Sulfabutin;Myelosan;Myeleukon;methanesulfonic acid tetramethylene ester;glyzophrol;Busulfanum;Bussulfam;NCI C01592;Myleran;Mylecytan;Myeloleukon;Milecitan;Mielosan |
| CAS号 : | 55-98-1 | |
| 货号 : | A593389 | |
| 分子式 : | C6H14O6S2 | |
| 纯度 : | 98% | |
| 分子量 : | 246.302 | |
| MDL号 : | MFCD00007562 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(203 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 |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+40% PEG300+water 10 mg/mL clear PO 0.5% CMC-Na 44 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Busulfan (BU), an alkylating agent that causes DNA damage by cross-linking DNAs and DNA and proteins, induces senescence in normal human diploid WI38 fibroblasts through the extracellular signal-regulated kinase (Erk) and p38 mitogen-activated protein kinase (p38 MAPK) cascade independent of the p53-DNA damage pathway[3]. 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 expression compared to the control[4]. Busulfan (2.5, 5.0 mg/kg, i.p.) causes earlier occurrence of persistent esturs in a dose dependent manner in rats. Busulfan (5.0 mg/kg) also increases the incidence of uterine adenocarcinomas and multiplicity of uterine neoplastic lesions. In addition, Busulfan decreases the serum 17β-estradiol(E2), progesterone and inhibin levels in rats, and elevates the E2/progesterone ratio only at 5.0 mg/kg[5]. IV busulfan is a convenient, safe, and effective conditioning agent used in HSCT (hematopoietic stem cell transplantation) that has a predictable pharmacokinetic profile[6]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| Kelly cells | 10-100 μM | Proliferation assay | 72 h | Antiproliferative activity against human Kelly cells at 10 to 100 uM after 72 hrs by MTT assay | 24814532 |
| LS cells | 10-100 μM | Proliferation assay | 72 h | Antiproliferative activity against human LS cells at 10 to 100 uM after 72 hrs by MTT assay | 24814532 |
| SiMa cells | 10-100 μM | Proliferation assay | 72 h | Antiproliferative activity against human SiMa cells at 10 to 100 uM after 72 hrs by MTT assay | 24814532 |
| 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 |
| NCT02114502 | Myeloma | Phase 2 | Withdrawn | - | - |
| NCT00997386 | Hematologic Neoplasms ... 展开 >> Multiple Myeloma Anemia, Aplastic Hemoglobinuria, Paroxysmal Myelofibrosis 收起 << | Phase 2 | Completed | - | United States, Arizona ... 展开 >> University Medical Center and UMC-North Clinic Tucson, Arizona, United States, 85719 收起 << |
| NCT01471444 | Disorder Related to Bone Marro... 展开 >>w Transplantation Leukemia Transplantation Infection 收起 << | Phase 3 | Active, not recruiting | November 1, 2020 | United States, Texas ... 展开 >> University of Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
4.06mL 0.81mL 0.41mL |
20.30mL 4.06mL 2.03mL |
40.60mL 8.12mL 4.06mL |
| 参考文献 |
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