Home>>Doxorubicinol (hydrochloride)

Doxorubicinol (hydrochloride) Sale

(Synonyms: 13-Dihydroadriamycin hydrochloride) 目录号 : GC43565

A doxorubicin metabolite

Doxorubicinol (hydrochloride) Chemical Structure

Cas No.:63950-05-0

规格 价格 库存 购买数量
500μg
¥1,284.00
现货
1mg
¥2,449.00
现货
5mg
¥11,564.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

客户使用产品发表文献 1

产品文档

Quality Control & SDS

View current batch:

产品描述

Doxorubicinol is the major metabolite of doxorubicin , an anthracycline antitumor antibiotic that inhibits DNA topoisomerase II by inducing double-stranded DNA breaks. Doxorubicinol is formed by NADPH-dependent reduction of the side chain carbonyl group of doxorubicin in human, rabbit, and canine cardiac tissue. Doxorubicinol inhibits sodium-potassium-dependent ATPase activity (IC50 = 5.40 μg/ml) and ATP-dependent calcium uptake (IC50= 4.5 μg/ml) in canine cardiac muscle and increases resting stress in contracting rabbit cardiac muscle. Clinically observed cardiotoxicities following doxorubicin treatment have been attributed to the formation and cardiac action of doxorubicinol.

Chemical Properties

Cas No. 63950-05-0 SDF
别名 13-Dihydroadriamycin hydrochloride
Canonical SMILES OC1=C(C[C@](C(O)CO)(O)C[C@@H]2O[C@@](O[C@@H](C)[C@H]3O)([H])C[C@@H]3N)C2=C(O)C(C4=O)=C1C(C5=CC=CC(OC)=C45)=O.Cl
分子式 C27H31NO11•HCl 分子量 582
溶解度 DMSO: Soluble,Methanol: Soluble 储存条件 Store at 4°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。
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。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 1.7182 mL 8.5911 mL 17.1821 mL
5 mM 0.3436 mL 1.7182 mL 3.4364 mL
10 mM 0.1718 mL 0.8591 mL 1.7182 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

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
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

Research Update

Development and Validation of Doxorubicin hydrochloride and Doxorubicinol Quantification Method in Dried Blood Spot by Liquid Chromatography-Tandem Mass Spectrometry

J Pharm Bioallied Sci 2020 Oct-Dec;12(4):406-412.PMID:33679086DOI:10.4103/jpbs.JPBS_167_20.

Dried blood spot as biosampling method offers a less invasive and easier procedure. This study aimed to develop the validated analytical method of doxorubicin hydrochloride and Doxorubicinol simultaneously in dried blood spot with hexamethylphosphoramide as the internal standard. A total of 30 μL blood was spotted on DBS paper and dried for 3 hours before it was extracted by protein precipitation method using water and methanol. The separation was performed on column Acquity UHPLC BEH C-18 (2.1 × 100 mm; 1.7 μm), with 0.15 mL/min flow rate and using 0.1% acetic acid and acetonitrile as mobile phase in gradient elution for 7 min. Quantification analysis was performed by a triple quadrupole mass spectrometry with electrospray ionization (ESI) in positive ion mode. The multiple reaction monitoring (MRM) was set at m/z 544.22 > 397.06 for doxorubicin hydrochloride; m/z 546.22 > 361.05 for Doxorubicinol; and m/z 180.03 > 135.16 for hexamethylphosphoramide. The lower limit of quantitation was 10 ng/mL for doxorubicin and 4 ng/mL for Doxorubicinol. Concentration range acquired was 10-200 ng/mL for doxorubicin and 4-100 ng/mL for Doxorubicinol. The precision and accuracy were within acceptable criteria of <15%. Dried blood spot samples acquired was stable for at least 30 days before analysis. This method fulfilled the validation requirement refers to Bioanalytical Method Validation Guideline of European Medicines Agency 2011 and US Food and Drug Administration 2018.

Direct quantitation of free, encapsulated, total doxorubicin and Doxorubicinol in stabilized frozen human plasma to support a BE study of liposomal doxorubicin

J Pharm Biomed Anal 2020 Sep 10;189:113388.PMID:32663760DOI:10.1016/j.jpba.2020.113388.

Regulatory guidance requires the quantification of encapsulated and free doxorubicin for a liposomal doxorubicin injection bioequivalence study. Due to the instability of liposome formulations in plasma samples, the release of free drug from the liposomal encapsulated doxorubicin during sample handling would result in elevation of measured free doxorubicin concentration. To prevent the potential release of free drug, stabilizer reagents and procedures were successfully developed and validated to adequately stabilize liposomal drugs in plasma samples during sample collection, storage and extraction. Three LC-MS/MS methods were developed and fully validated for direct quantitation of free, encapsulated and total doxorubicin concentrations in human plasma according to relevant regulatory guidance: Method 1: Quantitation of free doxorubicin and Doxorubicinol at a linear range of 1-400 ng/mL and 0.5-10 ng/mL, respectively, from stabilizer treated plasma samples using solid phase extraction (SPE); Method 2: Quantitation of encapsulated doxorubicin at a linear range of 50-50,000 ng/mL from the stabilizer treated plasma sample using SPE followed by PPE extraction method; Method 3: Quantitation of total concentration of doxorubicin from untreated plasma samples at a linear range of 50-50,000 ng/mL using PPE. All three methods were successfully used to support a bioequivalence study between Caelyx® and Duomeisu® (Doxorubicin hydrochloride Liposomal injection, generic doxorubicin formulation produced by CSPC). Incurred sample reanalysis (ISR) passing rate for total doxorubicin, free doxorubicin/Doxorubicinol, and encapsulated doxorubicin methods were 100 %, 84.7 %/100 %, and 98.5 %, respectively. The measured total doxorubicin concentrations matched the sum of free and encapsulated doxorubicin concentrations.

Doxorubicin pharmacokinetics following a single-dose infusion to sulphur-crested cockatoos (Cacatua galerita)

Aust Vet J 2004 Dec;82(12):769-72.PMID:15648940DOI:10.1111/j.1751-0813.2004.tb13246.x.

Objective: To determine the pharmacokinetics of doxorubicin in sulphur-crested cockatoos, so that its use in clinical studies in birds can be considered. Design: A pharmacokinetic study of doxorubicin, following a single intravenous (i.v.) infusion over 20 min, was performed in four healthy sulphur-crested cockatoos (Cacatua galerita). Procedure: Birds were anaesthetised and both jugular veins were cannulated, one for doxorubicin infusion and the other for blood collection. Doxorubicin hydrochloride (2 mg/kg) in normal saline was infused i.v. over 20 min at a constant rate. Serial blood samples were collected for 96 h after initiation of the infusion. Plasma doxorubicin concentrations were assayed using an HPLC method involving ethyl acetate extraction, reverse-phase chromatography and fluorescence detection. The limit of quantification was 20 ng/mL. Established non-parametric methods were used for the analysis of plasma doxorubicin data. Results: During the infusion the mean +/- SD for the Cmax of doxorubicin was 4037 +/- 2577 ng/mL. Plasma concentrations declined biexponentially immediately after the infusion was ceased. There was considerable intersubject variability in all pharmacokinetic variables. The terminal (beta-phase) half-life was 41.4 +/- 18.5 min, the systemic clearance (CI) was 45.7 +/- 18.0 mL/min/kg, the mean residence time (MRT) was 4.8 +/- 1.4 min, and the volume of distribution at steady state (V(SS)) was 238 +/- 131 mL/kg. The extrapolated area under the curve (AUC(0-infinity)) was 950 +/- 677 ng/mL x h. The reduced metabolite, Doxorubicinol, was detected in the plasma of all four parrots but could be quantified in only one bird with the profile suggesting formation rate-limited pharmacokinetics of Doxorubicinol. Conclusions and clinical relevance: Doxorubicin infusion in sulphur-crested cockatoos produced mild, transient inappetence. The volume of distribution per kilogram and terminal half-life were considerably smaller, but the clearance per kilogram was similar to or larger than reported in the dog, rat and humans. Traces of Doxorubicinol, a metabolite of doxorubicin, were detected in the plasma.