Dxd-d5(Synonyms: Exatecan-d5 derivative for ADC)

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Dxd-d5 (Synonyms: Exatecan-d5 derivative for ADC)

Dxd-D5 (Exatecan-D5 derivative for ADC) 是 Dxd 的氘代物。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。

Dxd-d5(Synonyms: Exatecan-d5 derivative for ADC)

Dxd-d5 Chemical Structure

规格 价格 是否有货 数量
1 mg ￥14500 In-stock
5 mg ￥40000 In-stock
10 mg ￥66500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

生物活性

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].

IC50 & Target

Topoisomerase I

0.31 μM (IC50)

体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

498.51

Formula

C26H19D5FN3O6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (200.60 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0060 mL 10.0299 mL 20.0598 mL
5 mM 0.4012 mL 2.0060 mL 4.0120 mL
10 mM 0.2006 mL 1.0030 mL 2.0060 mL

*

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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-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。
参考文献

  • [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.

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