Busulfan-d8
(Synonyms: 白消安 d8) 目录号 : GC46962
An internal standard for the quantification of busulfan
Cas No.:116653-28-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Busulfan-d8 is intended for use as an internal standard for the quantification of busulfan by GC- or LC-MS. Busulfan is an alkyl sulfonate that acts as an alkylating antineoplastic agent.1 It forms both intra- and interstrand crosslinks on DNA.2,3 In mammals, busulfan causes profound and prolonged reduction in the generation of hematopoietic progenitors without significantly affecting lymphocyte levels or humoral antibody responses.4
1.Appelbaum, F.R.Optimizing the conditioning regimen for acute myeloid leukemiaBest Pract.Res.Clin.Haematol.22(4)543-550(2009) 2.Iwamoto, T., Hiraku, Y., Oikawa, S., et al.DNA intrastrand cross-link at the 5'-GA-3' sequence formed by busulfan and its role in the cytotoxic effectCancer Science95454-458(2004) 3.Ponti, M., Souhami, R.L., Fox, B.W., et al.DNA interstrand crosslinking and sequence selectivity of dimethanesulphonatesBritish Journal of Cancer63(5)743-747(1991) 4.Copelan, E.A., and Deeg, H.J.Conditioning for allogeneic marrow transplantation in patients with lymphohematopoietic malignancies without the use of total body irradiationBlood80(7)1648-1658(1992)
| Cas No. | 116653-28-2 | SDF | |
| 别名 | 白消安 d8 | ||
| Canonical SMILES | CS(OC([2H])([2H])C([2H])([2H])C([2H])([2H])C([2H])([2H])OS(C)(=O)=O)(=O)=O | ||
| 分子式 | C6H6D8O6S2 | 分子量 | 254.3 |
| 溶解度 | DMF: 16.7 mg/ml,DMSO: 16.7 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml | 储存条件 | Store at -20°C,protect from light |
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.9324 mL | 19.6618 mL | 39.3236 mL |
| 5 mM | 0.7865 mL | 3.9324 mL | 7.8647 mL |
| 10 mM | 0.3932 mL | 1.9662 mL | 3.9324 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
A Simple Liquid Chromatography Tandem Mass Spectrometry Method for Quantitation of Plasma Busulfan
Methods Mol Biol 2016;1383:79-87.PMID:26660176DOI:10.1007/978-1-4939-3252-8_9.
Busulfan is an alkylating agent widely used in the ablation of bone marrow cells before hematopoietic stem cell transplant. Due to large intraindividual and interindividual variations, and narrow therapeutic window, therapeutic drug monitoring of busulfan is warranted. A quick and reliable HPLC-MS/MS method was developed for the assay of plasma busulfan. HPLC involved C18 column, and MS/MS was used in electrospray ionization (ESI) positive mode. Quantitation and identification of busulfan was made using various multiple reactions monitoring (MRMs). Isotopic labeled Busulfan-d8 was used as the internal standard. The method is linear from 50 to 2500 ng/mL and has with-in run and between-run imprecision of <10 %.
Fast and reliable quantification of busulfan in blood plasma using two-channel liquid chromatography tandem mass spectrometry: Validation of assay performance in the presence of drug formulation excipients
J Pharm Biomed Anal 2021 Sep 5;203:114216.PMID:34182411DOI:10.1016/j.jpba.2021.114216.
A fast and reliable method based on two-channel liquid chromatography coupled to tandem mass spectrometry was developed and successfully validated for quantification of busulfan. The drug vehicle polyethylene glycol 400 was quantified simultaneously in patient samples. The sample preparation consisted of simple protein precipitation using a mixture of methanol and zinc sulphate containing Busulfan-d8 as internal standard. Chromatographic separation was performed on a short biphenyl column (30 mm × 3.0 mm, 5 μm particles) using a step gradient from 30 % to 85 % methanol, ensuring co-elution of the analyte and internal standard. Quantification was performed using the mass transition of 264.1 > 151.1 for busulfan and 272.1 > 159.1 for the internal standard. Using only 20 μL of plasma sample, the lower limit of quantification was 25 ng/mL. Signal to noise ratio at the lower limit of quantification exceeded 300. The assay performance was not adversely affected by matrix effects originating from drug formulation excipients or other sample components. The coefficient of variation was ≤4 % and the mean accuracy 101-108 % across the calibration range 25-5 000 ng/mL. Chromatographic run time was 2 min and 8 s, allowing an effective run-time of 1 min and 10 s when using two alternating LC-channels. The assay has been implemented in routine practice with accreditation according to the ISO 15189 standard, and performs well in external quality control assessments. We present for the first time that shortly after an IV infusion of busulfan, the plasma levels of polyethylene glycol 400 may be in the range of 400-800 mg/L. The presence of these levels of detergent in patient samples may have detrimental effects on assay performance in LC-MS/MS, not limited to busulfan assays. This may be a concern for any LC-MS/MS analysis performed on samples collected within the first 24 h after an IV infusion of busulfan.
Quantification of busulfan in plasma by gas chromatography-mass spectrometry following derivatization with tetrafluorothiophenol
J Chromatogr B Biomed Sci Appl 1998 May 8;709(1):47-56.PMID:9653925DOI:10.1016/s0378-4347(98)00019-x.
A specific and highly sensitive method has been developed for the determination of busulfan in plasma by gas chromatography-mass spectrometry using a deuterium-labeled busulfan (Busulfan-d8) as internal standard. Plasma containing busulfan and Busulfan-d8 were extracted with ethyl acetate and derivatized with 2,3,5,6-tetrafluorothiophenol prior to the monitoring of specific ions. The limit of quantification of the assay was 20 ng/ml and the calibration curve was linear over the range of 10 to 2000 ng/ml of derivatized busulfan. This method was in good agreement with the GC-MS assay using derivatization with sodium iodide and measuring diiodobutane. In addition, a pharmacokinetic study of busulfan was conducted in six children. The apparent oral clearance was 5.7+/-1.9 ml/kg/min and the volume of distribution was 1.0+/-0.4 l/kg and were similar to those previously reported in pediatric patients.