Trastuzumab deruxtecan (solution)(Synonyms: DS-8201 (solution); DS-8201a (solution))

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Trastuzumab deruxtecan (solution) (Synonyms: DS-8201 (solution); DS-8201a (solution))

Trastuzumab deruxtecan (DS-8201a) (solution) 是一种抗人表皮生长因子受体 2 (HER2) 抗体-药物偶联物 (ADC)。Trastuzumab deruxtecan (solution) 由人源化抗 HER2 抗体，酶促裂解的肽接头和拓扑异构酶 I 抑制剂组成。Trastuzumab deruxtecan (solution) 可用于 HER2 阳性乳腺癌和胃癌的研究。

Trastuzumab deruxtecan (solution)(Synonyms: DS-8201 (solution); DS-8201a (solution))

Trastuzumab deruxtecan (solution) Chemical Structure

CAS No. : 1826843-81-5

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1mg (10 mg/mL * 100 μL in Aqueous solution) ￥8800 In-stock
5 mg (10 mg/mL * 500 μL in Aqueous solution) ￥20000 In-stock

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生物活性

Trastuzumab deruxtecan (DS-8201a) (solution) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan (solution) is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, and a topoisomerase I inhibitor. Trastuzumab deruxtecan (solution) can be used for the research of HER2-positive breast cancer and gastric cancer[1][2].

体外研究
(In Vitro)

Trastuzumab deruxtecan (1 pM-10 nM; 5 days) (solution) inhibits the growth of HER2-positive KPL-4 cells, with an IC50 of 109.7 pM[2].
Trastuzumab deruxtecan (10 nM; 5 days) (solution) shows bystander killing effects in HER2-negative MDA-MB-468 cells[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.

Cell Viability Assay[2]

Cell Line: KPL-4 and MDA-MB-468 cells
Concentration: 1, 10, 100, 1000, 10000 pM
Incubation Time: 5 days
Result: Killed both HER2-positive KPL-4 cells and HER2-negative MDA-MB-468 cells.

体内研究
(In Vivo)

Trastuzumab deruxtecan (3 mg/kg; a single i.v.) (solution) shows antitumor activity against not only HER2-positive tumors but also HER2-negative tumors under the co-inoculated condition[2].
Trastuzumab deruxtecan (10 mg/kg; i.v. on days 0 and 7) (solution) inhibits the tumor growth in in EMT6-hHER2 syngeneic mouse model[3].

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.

Animal Model: Female BALB/c nude mice injected with NCI-N87 and MDA-MB-468-Luc cells[2]
Dosage: 3 mg/kg
Administration: A single i.v.
Result: Almost all of the HER2-positive and HER-negative cells disappeared and there were little or no cancer cells remaining in the tumors.

Clinical Trial

CAS 号

1826843-81-5
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Kotani D, et, al. Trastuzumab deruxtecan for the treatment of patients with HER2-positive gastric cancer. Ther Adv Med Oncol. 2021 Jan 7;13:1758835920986518.

    [2]. Ogitani Y, et, al. Bystander killing effect of DS-8201a, a novel anti-human epidermal growth factor receptor 2 antibody-drug conjugate, in tumors with human epidermal growth factor receptor 2 heterogeneity. Cancer Sci. 2016 Jul;107(7):1039-46.

    [3]. Iwata TN, et, al. [Fam-] trastuzumab deruxtecan (DS-8201a)-induced antitumor immunity is facilitated by the anti-CTLA-4 antibody in a mouse model. PLoS One. 2019 Oct 1;14(10):e0222280.

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