Trastuzumab deruxtecan

CAS：1826843-81-5

品牌：MedChemExpress (MCE)

存储条件：Please store the product under the recommended conditions in the Certificate of Analysis.

生物活性：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)。曲妥珠单抗 deruxtecan 由人源化抗 HER2 抗体、酶促可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^[1][2]。

体外：Trastuzumab deruxtecan（1 pM-10 nM；5 天）抑制 HER2 阳性 KPL-4 细胞的生长，IC₅₀ 为 109.7 pM^[2]。< br/> Trastuzumab deruxtecan（10 nM；5 天）在 HER2 阴性 MDA-MB-468 细胞中表现出旁观者杀伤作用^[2]。

体内：Trastuzumab deruxtecan（3 mg/kg；单次静脉注射）在联合接种条件下不仅对 HER2 阳性肿瘤而且对 HER2 阴性肿瘤均显示出抗肿瘤活性^[2]。曲妥珠单抗deruxtecan（10 mg/kg；在第 0 天和第 7 天静脉注射）抑制 EMT6-hHER2 同基因小鼠模型中的肿瘤生长^[3]。

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.

[4]. Kumagai K, et al. Interstitial pneumonitis related to trastuzumab deruxtecan, a human epidermal growth factor receptor 2-targeting Ab-drug conjugate, in monkeys. Cancer Sci. 2020 Dec;111(12):4636-4645.