Product Description
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CellMosaic has designed this kit for label any antibody (IgG) 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 1 to 3 mg of one (CM11431x1) or three antibodies (CM11431x3).
If you have less amount of IgG, non-IgG type antibody, or other customization need, please select the customization radio button or fill out the information above.
Due to the unknown features of many customers’ antibodies, this kit is designed to have an average of 2-5 molecules of deruxtecan attached to each antibody molecule. Trastuzumab Deruxtecan, sold under the brand name Enhertu, has an average of 8 molecules of deruxtecan attached to each antibody molecule. If you are targeting higher loading and have not seen too many aggregations/precipitations with your antibody using this kit, please select the customization radio button for higher loading.
Drug Information
- Name: Deruxtecan (Mc-GGFG-DXd)
- Synonym: Exatecan derivative, DX 8951 derivative; DX8951 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 Antibody
- Preferably >90% pure by gel electrophoresis
- Total amount: 1-3 mg of protein content as measured by UV.
Key Features of this PerKit™
- Offers a simple and easy way to label IgG1 with Deruxtecan with minimum exposure to the toxin
- Enzymatic cleavable peptide linker GGFG
- Fast and easy preparation: 6 h preparation and <2 h hands-on time
- All reagents and supplies included for preparation and purification
- Easy to control the DAR if used together with the Thiol Assay Kit with Purification (Product#: CM90005)
- Over 90% conjugated products (free of unreacted drugs)
- 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.
Due to the unknown features of many customers’ antibodies, this kit is designed to have an average of 2-5 molecules of deruxtecan attached to each antibody molecule. Trastuzumab Deruxtecan, sold under the brand name Enhertu, has an average of 8 molecules of deruxtecan attached to each antibody molecule. If you are targeting higher loading and have not seen too many aggregations/precipitations with your antibody using this kit, please contact CellMosaic for supplying a modified kit for high loading.
Conjugation Chemistry
Schematic diagram of the workflow for preparing antibody-Deruxtecan conjugates starting with 3 mg of IgG (volume of reagents varies if the amount of IgG is < 3 mg
Related Products
Thiol Assay Kit with Purification (Product #: CM90005): The reducing protocol is optimized for monoclonal IgG1 subtype to obtain an average 4 thiols per antibody (DAR = 4). For other IgG subtypes or polyclonal antibodies, the DAR may vary. For the best performance of the ADC and to obtain the desired DAR, you can purchase this kit separately and use it to perform an in-process thiol assay after the antibody reduction (Step C5 Note Section). The amount of reducing reagent can be adjusted based on the data to obtain your desired DAR.
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.
