CellMosaic® has designed this kit for label any protein (≥20 KDa) with Deruxtecan. Deruxtecan is an exatecan-derivative topoisomerase I inhibitor (DXd) with an enzymatically cleavable peptide linker GGFG (Nakada, T. et. al. Bioorg. Med. Chem. Lett. 2016, 26, 1542−1545). The user supplies the antibody. The kit includes Deruxtecan with an maleimide active group, which can be coupled directly to the antibody after reduction through alkylation in a single step. The product is purified to remove any unreacted drugs.
Kit is configured to conjugate 6.67-20 nano-mole (nmol) of one (CM11432x1) or three proteins (CM11432x3).
If you have a smaller amount of protein, a protein with a MW below 20KDa, or other customization needs, please select the customization radio button and/or fill out the information above.
- Name: Deruxtecan (Mc-GGFG-DXd)
- Synonym: Exatecan derivative, DX 8951 derivative; DXd; payload for DS-8201a;
- CAS number: 1599440-13-7
- Chemical formula: C52H56FN9O13
- MW: 1034.0684
- Mechanism of action: Trastuzumab Deruxtecan, sold under the brand name Enhertu was approved by US FDA for treating metastatic HER2-postive breast cancer.
Requirement for Protein
- Preferably >90% pure by gel electrophoresis
- Total amount: 6.67-20 nano-mole (nmol) protein content as measured by UV.
Key Features of this PerKit™
- Offers a simple and easy way to label protein with Deruxtecan with minimal exposure to the toxin
- Enzymatic cleavable peptide linker GGFG
- Fast and easy preparation: 6 h preparation and <2 hours of hands-on time
- All reagents and supplies included for preparation and purification
- Options to choose tailored services at CellMosaic® after conjugation
After conjugation: you can choose to send your sample to CellMosaic® for HPLC analysis and determination of the DAR.
Schematic diagram of the workflow for preparing protein-Deruxtecan conjugates starting with 20 nmol of protein (volume of reagents varies if the amount of protein is < 20 nmol and MW is <60 KDa).
Hydrophobic Interaction Chromatography (HIC) Buffer Set (Product#: CM02025): For ADCs prepared via a reduced thiol of the antibody, HIC HPLC is used to calculate the DAR and the heterogeneity of the ADCs. The conjugates are separated based on hydrophobicity. Antibodies loaded with the same number of drugs (same DAR) will have similar hydrophobicity and be eluted as a single peak. CellMosaic® offers HIC buffer for our customers to use with any HIC column. The CM02025 product sheet contains all of the information and methodology needed to run an HIC HPLC analysis. If you do not have access to an HPLC facility, you can send your sample to CellMosaic® for analysis.
Size Exclusion Chromatography (SEC) HPLC Protein Standards (Product #: CM92004 and CM92005): SEC HPLC separates the conjugates by apparent molecular weight (MW) or size in aqueous solution. The larger the MW of the conjugate, the earlier it elutes. By comparing the SEC profile of unlabeled IgG and the ADC, you can estimate how much aggregation is in the ADC. CellMosaic® offers two SEC standards for our customers to use with any SEC column. The CM92004 product sheet contains all of the information and methodology you need to run an SEC HPLC analysis. If you do not have access to an HPLC facility, you can send your sample to CellMosaic® for analysis.
ADC stabilizing PBS buffer (5x) (Product #: CM02022): CM02022 contains 5x PBS buffer and other stabilizers to prevent the hydrophobic drugs from interacting with each other during storage, which would cause the ADCs to precipitate out. Stabilization buffer also helps preserve the structure of the ADCs during lyophilization. The buffer is biocompatible and can be used directly for any in vitro and in vivo studies.