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MedChemExpress - Model Trastuzumab deruxtecan -1826843-81-5
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, a topoisomerase I inhibitor (a toxin component of Dxd). Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer[1][2].MCE products for research use only. We do not sell to patients.
Trastuzumab deruxtecan
MCE China：Trastuzumab deruxtecan
Brand：MedChemExpress (MCE)
Cat. No.HY-138298A
CAS：1826843-81-5
Synonyms：DS-8201; DS-8201a
Purity：99.58%
Storage：-80°C, protect from light
Shipping：Shipping with dry ice.
Description：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, a topoisomerase I inhibitor (a toxin component of Dxd). Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer.
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[2].Trastuzumab deruxtecan (10 nM; 5 days) shows bystander killing effects in HER2-negative MDA-MB-468 cells[2].
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[2].Trastuzumab deruxtecan (10 mg/kg; i.v. on days 0 and 7) inhibits the tumor growth in in EMT6-hHER2 syngeneic mouse model[3].
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References：
[1]. 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. [Content Brief]
[2]. 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. [Content Brief]
[3]. 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. [Content Brief]
[4]. 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. [Content Brief]
Brand introduction:
• MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
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