2. Antibody-drug Conjugate/ADC Related Immunology/Inflammation Cell Cycle/DNA Damage Apoptosis
  3. Antibody-Drug Conjugates (ADCs) Mucin Topoisomerase Apoptosis
  4. DS-3939a

DS-3939a (DS-3939) 是一种抗 TA-MUC1的抗体偶联药物 (ADC)。DS-3939a 由人源化抗 TA-MUC1 IgG1 单克隆抗体 Gatipotuzumab (HY-P99634)、一种稳定且可切割的基于四肽的连接子 (Gly-Gly-Phe-Gly)、以及 DNA 拓扑异构酶 I 抑制剂有效载荷 (DXd) (HY-13631D) 组成，其用于 ADC 的药物-连接子偶联物为 Exatecan (HY-13631)。DS-3939a 通过诱导 DNA 损伤和凋亡 (apoptosis)，抑制 TA-MUC1 阳性癌细胞 (CFPAC-1, NCI-H2110) 的生长。DS-3939a 在多种 TA-MUC1 表达的晚期实体瘤中表现出显著的抗肿瘤活性。DS-3939a 可用于研究 TA-MUC1 表达的晚期癌症。

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DS-3939a

DS-3939a Chemical Structure

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DS-3939a 相关抗体

Top Publications Citing Use of Products

查看 Mucin 亚型特异性产品:

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MUC1

查看 Topoisomerase 亚型特异性产品:

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Topoisomerase Topo I Topo II

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DS-3939a (DS-3939) is an anti-TA-MUC1 (tumor-associated mucin-1) antibody-drug conjugate (ADC). DS-3939a consists of a humanized anti-TA-MUC1 IgG1 monoclonal antibody Gatipotuzumab ( HY-P99634), a stable and cleavable tetrapeptide-based linker (Gly-Gly-Phe-Gly), and a DNA topoisomerase I inhibitor payload (DXd) (HY-13631D), and the drug-linker conjugate for ADC is Exatecan (HY-13631). DS-3939a inhibits the growth of TA-MUC1-positive cancer cells (CFPAC-1, NCI-H2110) by inducing DNA damage and apoptosis. DS-3939a exhibits significant antitumor activity in a variety of TA-MUC1-expressing advanced solid tumors. DS-3939a can be used for the study of TA-MUC1-expressing advanced cancers[1].

IC50 & Target[1]

MUC1

 

Topoisomerase I

 

体外研究
(In Vitro)

DS-3939a (0.01-10000 ng/mL, 6 d) 抑制 TA-MUC1 阳性 CFPAC-1 和 NCI-H2110 细胞的生长[1]。
DS-3939a (3 μg/mL, 2 d) 上调 TA-MUC1 阳性 CFPAC-1 细胞中 γH2AX 和 cleaved PARP 的表达[1]。

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

DS-3939a 相关抗体:

Western Blot Analysis[1]

Cell Line: TA-MUC1-positive CFPAC-1 cells
Concentration: 3 μg/mL
Incubation Time: 2 d
Result: Upregulated the expression of γH2AX and cleaved PARP in TA-MUC1-positive CFPAC-1 cells.
体内研究
(In Vivo)

DS-3939a (0.25-8 mg/kg, 静脉注射, 第 0 天给药一次) 在携带 CFPAC-1 胰腺癌异种移植瘤的雌性裸鼠中表现出剂量依赖性的抑瘤作用[1]。
DS-3939a (10 mg/kg, 静脉注射, 第 0 天给药一次) 在 TA-MUC1 阳性的 NCI-H2110 肺癌异种移植瘤中表现出显著的抗肿瘤活性，但在 TA-MUC1 阴性的 HCT-15 结直肠癌异种移植瘤的雌性裸鼠中无作用[1]。

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

Animal Model: CFPAC-1 pancreatic cancer cells (1.0×107 cells in 0.1 mL saline) were subcutaneously implanted into the right flanks of 4-5-week-old female nude mice[1]
Dosage: 0.25, 0.5, 1, 2, 4, 8 mg/kg
Administration: i.v., once on day 0
Result: Achieved dose-dependent tumor growth inhibition.
Animal Model: NCI-H2110 lung cancer cells or HCC70 triple-negative breast cancer cells were subcutaneously implanted into the flanks of 4-5-week-old female nude mice[1]
Dosage: 10 mg/kg
Administration: i.v., once on day 0
Result: Exerted potent antitumor activity against TA-MUC1-positive NCI-H2110 lung cancer xenografts but no effect on TA-MUC1-negative HCT-15 colorectal cancer xenografts.
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

DS-3939a 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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:

DS-3939aDS-3939DS3939DS 3939Antibody-Drug Conjugates (ADCs)MucinTopoisomeraseApoptosisAntibody-Drug Conjugatesantibody-drug conjugateMUC1cancersapoptosisInhibitorinhibitorinhibit

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