Busulfan
(Synonyms: 白消安) 目录号 : GC13671
Busulfan是一种烷化剂，可通过烷基化作用修饰DNA，对human serum Paraoxonase 1的IC50值为77μM。
Cas No.:55-98-1
Sample solution is provided at 25 µL, 10mM.
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Busulfan is an alkylating drug alkylates DNA, with an IC50 value of 77μM for human serum Paraoxonase 1[1]. Busulfan has been widely used in cellular and animal models to induce rapidly dividing cell death[2].
In vitro, Busulfan treatment in P39 cells at 100μg/ml for 8 hours induced apoptosis, accompanied by caspase activation and cleavage of Bcl-2 and PARP proteins[3]. Treatment of HepaRG cells with 1000μM Busulfan for 4 days resulted in cellular mitochondrial dysfunction, elevated neutral lipid levels, increased fatty acid uptake, and decreased secretion of very-low-density lipoprotein[4]. Treatment of U2OS and MG-63 cells with 150μM Busulfan for 48 hours significantly inhibited cell viability, up-regulated the miR-200 family and regulated related target genes[5]. Treatment with 100μM Busulfan for 48 hours inhibited autophagy in mouse spermatogonial progenitor cells, resulting in a significant up-regulation of mTOR phosphorylation at Ser2448[6].
In vivo, Busulfan treatment via a single intraperitoneal injection at the dose of 40mg/kg for 56 days caused male C3H/Kam mice permanently infertile and led to the morphological damage to sperm produced by surviving stem cell spermatogonia[7]. In NOD/ LtSz-scid /IL2Rγ knockout mice, two intraperitoneal injections of 25mg/kg Busulfan at 48 and 24 hours before infusion of human cells promoted engraftment of human hematopoietic stem cell (HSC) and significantly improved survival[8].
References:
[1] Söyüt H. Investigation of inhibition of busulfan (Chemotherapeutic Drug) on human serum paraoxonase-1 (PON1)[J]. Int. J. Pharmacol. 2021, 17(8), 572–576.
[2] Berger D P, Winterhalter B R, Dengler W A, et al. Preclinical activity off hepsulfam and busulfan in solid human tumor xenografts and human bone marrow[J]. Anti-Cancer Drugs, 1992, 3(5): 531-540.
[3] Hassan Z, Hassan M, Hellström-Lindberg E. The pharmacodynamic effect of busulfan in the P39 myeloid cell line in vitro[J]. Leukemia, 2001, 15(8): 1240-1247.
[4] Allard J, Bucher S, Ferron P J, et al. Busulfan induces steatosis in HepaRG cells but not in primary human hepatocytes: Possible explanations and implication for the prediction of drug‐induced liver injury[J]. Fundamental & Clinical Pharmacology, 2024, 38(1): 152-167.
[5] Mei Q, Li F, Quan H, et al. Busulfan inhibits growth of human osteosarcoma through miR‐200 family micro RNA s in vitro and in vivo[J]. Cancer science, 2014, 105(7): 755-762.
[6] Wei R, Zhang X, Cai Y, et al. Busulfan suppresses autophagy in mouse spermatogonial progenitor cells via mTOR of AKT and p53 signaling pathways[J]. Stem Cell Reviews and Reports, 2020, 16(6): 1242-1255.
[7] Bucci L R, Meistrich M L. Effects of busulfan on murine spermatogenesis: cytotoxicity, sterility, sperm abnormalities, and dominant lethal mutations[J]. Mutation Research/Fundamental and Molecular Mechanisms of Mutagenesis, 1987, 176(2): 259-268.
[8] Hayakawa J, Hsieh M M, Uchida N, et al. Busulfan produces efficient human cell engraftment in NOD/LtSz-Scid IL2Rγ null mice[J]. Stem cells, 2009, 27(1): 175-182.
Busulfan是一种烷化剂，可通过烷基化作用修饰DNA，对human serum Paraoxonase 1的IC50值为77μM[1]。Busulfan广泛应用于细胞和动物模型中诱导快速分裂细胞死亡[2]。
在体外，100μg/ml的Busulfan处理P39细胞8小时可诱导细胞凋亡，伴随caspase激活及Bcl-2和PARP蛋白裂解[3]。1000μM的Busulfan处理HepaRG细胞4天会导致细胞线粒体功能障碍、中性脂质水平升高、脂肪酸摄取增加及极低密度脂蛋白分泌减少[4]。150μM的Busulfan处理U2OS和MG-63细胞48小时能显著抑制细胞活力，上调miR-200家族并调控相关靶基因[5]。100μM的Busulfan处理小鼠精原祖细胞48小时可抑制自噬过程，显著增强mTOR Ser2448位点磷酸化[6]。
在体内，Busulfan以40mg/kg的剂量单次腹腔注射（56天后）导致雄性C3H/Kam小鼠永久性不育，并导致存活的干细胞精原细胞产生的精子发生形态损伤[7]。NOD/LtSz-scid/IL2Rγ敲除小鼠在输注人细胞前48小时和24小时两次腹腔注射25mg/kg剂量的Busulfan，可促进人造血干细胞（HSC）植入并显著提高生存率[8]。
| Cell experiment [1]: | |
Cell lines | P39 cells |
Preparation Method | P39 cells were cultured in RPMI 1640 medium supplemented with 10% heat-inactivated fetal bovine serum (FBS), penicillin (25IU/ml), and streptomycin (25μg/ml) at 37°C and 5% CO2 humidity. The cell seeding concentration was 0.20 × 106 cells /ml. All experiments were performed in exponentially growing cells. Cells were incubated with Busulfan at a final concentration of 10, 20, 40, 60, 80, and 100μg/ml for 2, 4, and 8 hours. The cells were washed and re-cultured for 72h in medium without Busulfan. In all experiments, cells cultured in medium supplemented with 10% FBS or medium supplemented with 10% FBS and 0.5% DMSO were used as controls. Cells treated with etoposide at a final concentration of 6μg/ml were used as a positive control for apoptosis. Cell number and viability were determined by the trypan blue exclusion assay. |
Reaction Conditions | 10, 20, 40, 60, 80, and 100μg/ml; 2, 4, and 8h |
Applications | Busulfan inhibited cell viability and reduced cell number in a concentration and time-dependent manner within P39 cells. |
| Animal experiment [2]: | |
Animal models | Wistar rats |
Preparation Method | Thirty-two male Wistar rats (6-8 weeks old, with an average body weight of 150g) were housed under standard conditions (22 ± 3℃, humidity 45-60%), and had unlimited access to water and chewable food. The rats were randomly divided into 2 groups (8 rats in each group); (I): The control group of rats received no injections; (II): The rats in the second group were intraperitoneally injected with 40mg/kg Busulfan once. Samples were taken from the rats 56 days after the injection, and the histopathological changes were analyzed. |
Dosage form | 40mg/kg for once; i.p. |
Applications | Busulfan treatment led to the depletion and destruction of sperm formation in rats, with congestion in the kidney tissue and extensive necrosis, degeneration and formation of hyaline casts in the renal tubules. |
References: | |
| Cas No. | 55-98-1 | SDF | |
| 别名 | 白消安 | ||
| 化学名 | 4-methylsulfonyloxybutyl methanesulfonate | ||
| Canonical SMILES | CS(=O)(=O)OCCCCOS(=O)(=O)C | ||
| 分子式 | C6H14O6S2 | 分子量 | 246.3 |
| 溶解度 | ≥ 12.3mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.0601 mL | 20.3004 mL | 40.6009 mL |
| 5 mM | 812 μL | 4.0601 mL | 8.1202 mL |
| 10 mM | 406 μL | 2.03 mL | 4.0601 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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