Trastuzumab deruxtecan  (Synonyms: DS-8201; DS-8201a)

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

153000 (average)

1826843-81-5

Solid

White to off-white

[Trastuzumab deruxtecan]

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

• [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]