Trastuzumab deruxtecan (Synonyms: DS-8201; DS-8201a)
目录号: PL03733 纯度: ≥99%
CAS No. :1826843-81-5
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中文名称
Trastuzumab deruxtecan
英文名称
Trastuzumab deruxtecan
英文别名
Trastuzumab deruxtecan;Trastuzumab deruxtecan (solution)
Cas No.
1826843-81-5
包装储存
Please store the product under the recommended conditions in the Certificate of Analysis.
产品详情
Trastuzumab deruxtecan (DS-8201a) 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 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 可用于 HER2 阳性乳腺癌和胃癌的研究。
生物活性
Trastuzumab deruxtecan (DS-8201a) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, and a topoisomerase I inhibitor. Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer.
性状
Solid
体外研究(In Vitro)
Trastuzumab deruxtecan (1 pM-10 nM; 5 days) inhibits the growth of HER2-positive KPL-4 cells, with an IC50 of 109.7 pM.
Trastuzumab deruxtecan (10 nM; 5 days) shows bystander killing effects in HER2-negative MDA-MB-468 cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Trastuzumab deruxtecan (3 mg/kg; a single i.v.) shows antitumor activity against not only HER2-positive tumors but also HER2-negative tumors under the co-inoculated condition.
Trastuzumab deruxtecan (10 mg/kg; i.v. on days 0 and 7) inhibits the tumor growth in in EMT6-hHER2 syngeneic mouse model. has not independently confirmed the accuracy of these methods. They are for reference only.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
ClinicalTrial
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.
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