Trastuzumab deruxtecan

MCE 國際站：Trastuzumab deruxtecan

CAS：1826843-81-5

品牌：MedChemExpress (MCE)

存儲條件：Please store the product under the recommended conditions in the Certificate of Analysis.

生物活性：Trastuzumab deruxtecan (DS-8201a) 是一種抗人表皮生長因子受體 2 (HER2) 抗體-藥物偶聯物 (ADC)。曲妥珠單抗 deruxtecan 由人源化抗 HER2 抗體、酶促可裂解的肽接頭和拓撲異構酶 I 抑制劑組成。 Trastuzumab deruxtecan可用于HER2陽性乳腺癌和胃癌的研究^[1][2]。

^{_{體外：Trastuzumab deruxtecan（1 pM-10 nM；5 天）抑制 HER2 陽性 KPL-4 細胞的生長，IC50 為 109.7 pM[2]。< br/> Trastuzumab deruxtecan（10 nM；5 天）在 HER2 陰性 MDA-MB-468 細胞中表現出旁觀者殺傷作用[2]。}}

體內：Trastuzumab deruxtecan（3 mg/kg；單次靜脈注射）在聯合接種條件下不僅對 HER2 陽性腫瘤而且對 HER2 陰性腫瘤均顯示出抗腫瘤活性^[2]。
曲妥珠單抗deruxtecan（10 mg/kg；在第 0 天和第 7 天靜脈注射）抑制 EMT6-hHER2 同基因小鼠模型中的腫瘤生長^[3]。

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研究領域：Antibody-drug Conjugate/ADC Related  |  Protein Tyrosine Kinase/RTK  |  JAK/STAT Signaling

作用靶點：Antibody-Drug Conjugates (ADCs)  |  EGFR

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參考文獻：

[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.