1826843-81-5

1826843-81-5 structure
1826843-81-5 structure
  • Name: Trastuzumab deruxtecan
  • Chemical Name: Trastuzumab deruxtecan
  • CAS Number: 1826843-81-5
  • Molecular Formula:
  • Molecular Weight:
  • Catalog: Signaling Pathways JAK/STAT Signaling EGFR
  • Create Date: 2021-07-27 12:46:14
  • Modify Date: 2024-01-05 03:34:31
  • 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, and a topoisomerase I inhibitor. Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer[1][2].

Name Trastuzumab deruxtecan
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, and a topoisomerase I inhibitor. Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer[1][2].
Related Catalog
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]. Cell Viability Assay[2] Cell Line: KPL‐4 and MDA‐MB‐468 cells Concentration: 1, 10, 100, 1000, 10000 pM Incubation Time: 5 days Result: Killed both HER2‐positive KPL‐4 cells and HER2‐negative MDA‐MB‐468 cells.
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]. Animal Model: Female BALB/c nude mice injected with NCI‐N87 and MDA‐MB‐468‐Luc cells[2] Dosage: 3 mg/kg Administration: A single i.v. Result: Almost all of the HER2‐positive and HER‐negative cells disappeared and there were little or no cancer cells remaining in the tumors.
References

[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.

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