详情描述
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.
Product information
CAS Number: 1826843-81-5
Molecular Weight: 493.48
Formula: C26H24FN3O6
Synonym:
DS-8201
DS-8201a
Chemical Name: N-(10-ethyl-18-fluoro-10-hydroxy-19-methyl-5, 9-dioxo-8-oxa-4, 15-diazahexacyclo[14.7.1.02, 14.04, 13.06, 11.020, 24]tetracosa-1, 6(11), 12, 14, 16, 18, 20(24)-heptaen-23-yl)-2-hydroxyacetamide
Smiles: CC1C2CCC(NC(=O)CO)C3=C4CN5C(=CC6=C(COC(=O)C6(O)CC)C5=O)C4=NC(=CC=1F)C3=2
InChiKey: PLXLYXLUCNZSAA-UHFFFAOYSA-N
InChi: InChI=1S/C26H24FN3O6/c1-3-26(35)15-6-19-23-13(8-30(19)24(33)14(15)10-36-25(26)34)22-17(28-20(32)9-31)5-4-12-11(2)16(27)7-18(29-23)21(12)22/h6-7,17,31,35H,3-5,8-10H2,1-2H3,(H,28,32)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. Trastuzumab deruxtecan (10 nM; 5 days) shows bystander killing effects in 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. Trastuzumab deruxtecan (10 mg/kg; i.v. on days 0 and 7) inhibits the tumor growth in in EMT6-hHER2 syngeneic mouse model.
References:
- 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.
- 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.
Products are for research use only. Not for human use.