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MCE 国际站：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]。
热销产品：DiR | IL-13, Mouse | C75 | Abiraterone acetate | Cl-amidine (hydrochloride) | Resiniferatoxin | MSOP | Ampicillin | Nirmatrelvir | Gentamicin (sulfate)
研究领域：Antibody-drug Conjugate/ADC Related | Protein Tyrosine Kinase/RTK | JAK/STAT Signaling
作用靶点：Antibody-Drug Conjugates (ADCs) | EGFR
Trending products：Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
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.
