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(lián)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?fù)洚悩?gòu)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(xì)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(xì)胞中表現(xiàn)出旁觀者殺傷作用[2]。
體內(nèi):Trastuzumab deruxtecan(3 mg/kg;單次靜脈注射)在聯(lián)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]。
熱銷產(chǎn)品:DiR | IL-13, Mouse | C75 | Abiraterone acetate | Cl-amidine (hydrochloride) | Resiniferatoxin | MSOP | Ampicillin | Nirmatrelvir | Gentamicin (sulfate)
研究領(lǐng)域:Antibody-drug Conjugate/ADC Related | Protein Tyrosine Kinase/RTK | JAK/STAT Signaling
作用靶點:Antibody-Drug Conjugates (ADCs) | EGFR
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
參考文獻(xiàn):
[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.
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