HRP-Deruxtecan (Dxd) (1:1) Conjugate

Product Description

Deruxtecan is an exatecan (Exa) derivative appended with a cleavable peptide linker. It is a very potent inhibitor of topoisomerase I and an anticancer agent. Deruxtecan is used to prepare antibody-drug conjugates (ADCs), such as trastuzumab Deruxtecan (T-DXd, also known as Enhertu®, Daiichi Sankyo), targeting HER2. Deruxtecan is approved in HER2-expressing breast (BC) and gastric (GC) cancers. This HRP-Deruxtecan conjugate is designed with similar linker chemistry as ADCs and PDCs prepared by our customer using our Antibody Deruxtecan Conjugation Kit (Cat#: CM11431) and our Protein Deruxtecan Conjugation Kit (Cat#: CM11432).  This conjugate is synthesized at CellMosaic for our customer's use in horseradish peroxidase (HRP) based assays. A long flexible PEG linker is also incorporated in the conjugate to retain HRP activity and Deruxtecan binding. The final conjugate is HPLC-purified to obtain 1:1 Deruxtecan-labeled HRP and is lyophilized from PBS buffer containing sugar-based stabilizer for easy shipping and storage.

The product is sold as 1 vial of 0.5 mg (Cat# CM53215-0.5MG) or 4 vials of 0.5 mg (Cat# CM53215-2MG). For bulk orders beyond this range, please contact us for a quote.

Application

• Assay development for the quantitation and detection of Deruxtecan labeled biopolymers (ADCs and PDCs) and Deruxtecan drug released from the conjugate.
• Indirect and competitive ELISA assay

Key Features

• Lyophilized powder is ready for usage after reconstitution with water, no need for external buffer.
• HPLC-purified single-labeled conjugate, 1:1 HRP-Deruxtecan
• Retained HRP activity, 200-300 units/mg protein (1 unit is the amount of enzyme that will form 1.0 mg purpurogallin from pyrogallol in 20s at pH 6.0 at 20°C).
• A long flexible PEG linker incorporated to retain the HRP activity and Deruxtecan binding.

Selected References for Deruxtecan ADC

1) Takashi Nakada, et al. Novel antibody drug conjugates containing exatecan derivative-based cytotoxic payloads. Bioconjugic & Medicinal Chem. Lett. 2016;26: 1542–45.

2) Yusuke Ogitani, 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;107(7):1039−46.

3) Naoki Takegawa, et al. DS-8201a, a new HER2-targeting antibody-drug conjugate incorporating a novel DNA topoisomerase I inhibitor, overcomes HER2-positive gastric cancer T-DM1 resistance. Int. J. Cancer. 2017;141:1682-89.