2. Cell Cycle/DNA Damage Antibody-drug Conjugate/ADC Related
  3. Topoisomerase ADC Cytotoxin
  4. Dxd

Dxd  (Synonyms: Exatecan derivative for ADC)

目录号: HY-13631D 纯度: ≥99.0%
COA 产品使用指南

摩尔计算器

Dxd (Exatecan derivative for ADC) 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。

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Dxd Chemical Structure

Dxd Chemical Structure

CAS No. : 1599440-33-1

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1520
In-stock
1 mg ￥1142
In-stock
5 mg ￥1400
In-stock
10 mg ￥1960
In-stock
50 mg ￥3000
In-stock
100 mg ￥4000
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Dxd:

Dxd 相关抗体

Top Publications Citing Use of Products

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Topoisomerase Topo I Topo II

查看 ADC Cytotoxin 亚型特异性产品:

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Auristatin Calicheamicins Camptothecins Daunorubicins/Doxorubicins Duocarmycins Maytansinoids Pyrrolobenzodiazepines Traditional Cytotoxic Agents

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Dxd (Exatecan derivative for ADC) 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).

IC50 & Target[1]

Topoisomerase I

0.31 μM (IC50)

Camptothecins

 

体外研究
(In Vitro)

Dxd (Exatecan derivative for ADC) 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). Dxd is cytotoxic to human cancer cell lines of KPL-4, NCI-N87, SK-BR-3, and MDA-MB-468 with IC50s of 1.43 nM-4.07 nM, but the control IgG-ADC (Dxd is the payload) shows no inhibition on the four cell lines (with HER2 expression). DS-8201a (Dxd is the payload) displays significant suppression on the HER2-positive KPL-4, NCI-N87, and SK-BR-3 cell lines, with IC50 values of 26.8, 25.4, and 6.7 ng/mL, respectively, but with no such inhibition on MDA-MB-468 (IC50, >10,000 ng/mL)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Dxd 相关抗体:
体内研究
(In Vivo)

DS-8201a (Dxd is the payload, 10 mg/kg, i.v.) shows potent antitumor activity in HER2-positive models with KPL4, JIMT-1, and Capan-1 and in HER2 low-expressing ST565 and ST313 models with HER2 IHC 1+/FISH-negative expression[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

493.48

Formula

C26H24FN3O6
CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 40 mg/mL (81.06 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0264 mL 10.1321 mL 20.2642 mL
5 mM 0.4053 mL 2.0264 mL 4.0528 mL
查看完整储备液配制表

* 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。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: ≥99.0%

COA (205 KB) HNMR (266 KB) LCMS (94 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[1]

Cells are seeded to a 96-well plate at 1,000 cells per well. After overnight incubation, Dxd is added. Cell viability is evaluated after 6 days using a CellTiter-Glo Luminescent Cell Viability Assay. For the detection of HER2 expression in each cell line, cells are incubated on ice for 30 minutes with FITC Mouse IgG1, κ Isotype Control, or anti-HER2/neu FITC. After washing, the labeled cells are analyzed by FACSCalibur. Relative mean fluorescence intensity (rMFI) is calculated[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Briefly, each cell suspension or tumor fragment is inoculated subcutaneously into specific pathogen-free female nude mice. When the tumor has grown to an appropriate volume, the tumor-bearing mice are randomized into treatment and control groups based on the tumor volumes, and dosing is initiated on day 0. Each substance (DS-8201a, 1 or 10 mg/kg, i.v.; Dxd is the payload) is administered intravenously to the mice. Tumor growth inhibition (TGI, %) is calculated[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

Dxd 相关分类

完整储备液配制表

* 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。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0264 mL 10.1321 mL 20.2642 mL 50.6606 mL
5 mM 0.4053 mL 2.0264 mL 4.0528 mL 10.1321 mL
10 mM 0.2026 mL 1.0132 mL 2.0264 mL 5.0661 mL
15 mM 0.1351 mL 0.6755 mL 1.3509 mL 3.3774 mL
20 mM 0.1013 mL 0.5066 mL 1.0132 mL 2.5330 mL
25 mM 0.0811 mL 0.4053 mL 0.8106 mL 2.0264 mL
30 mM 0.0675 mL 0.3377 mL 0.6755 mL 1.6887 mL
40 mM 0.0507 mL 0.2533 mL 0.5066 mL 1.2665 mL
50 mM 0.0405 mL 0.2026 mL 0.4053 mL 1.0132 mL
60 mM 0.0338 mL 0.1689 mL 0.3377 mL 0.8443 mL
80 mM 0.0253 mL 0.1267 mL 0.2533 mL 0.6333 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dxd1599440-33-1Exatecan derivative for ADCTopoisomeraseADC CytotoxinADC PayloadHER2-targetingADCInhibitorinhibitorinhibit

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