您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Dxd-D5
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Dxd-D5
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Dxd-D5图片
规格:98%
分子量:498.51
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
Dxd-D5 (Exatecan-D5 derivative for ADC) 是 Dxd 的氚代物。Dxd 是一种有效的 DNA topoisomerase I 抑制剂,IC50 值为 0.31 μM,可用作靶作用于 HER2 的抗体偶联药物 ADC (DS-8201a) 的有效载荷。
货号:ajcx33276
CAS:N/A
分子式:C26H19D5FN3O6
分子量:498.51
溶解度:DMSO : 100 mg/mL (200.60 mM; ultrasonic and warming and heat to 60°C)
纯度:98%
存储:Store at -20°C
库存:现货

Background:

Dxd-D5 (Exatecan-D5 derivative for ADC) is a deuterium labeled Dxd. Dxd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) [1].

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[2].

[1]. Ogitani Y, et al. DS-8201a, A Novel HER2-Targeting ADC with a Novel DNA Topoisomerase I Inhibitor, Demonstrates a Promising Antitumor Efficacy with Differentiation from T-DM1. Clin Cancer Res. 2016 Oct 15;22(20):5097-5108.
[2]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.