Product Description
CellMosaic® has designed this kit to label any antibody (IgG) with Deruxtecan.
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Deruxtecan is an exatecan-derivative topoisomerase I inhibitor (DXd) featuring 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 a maleimide active group, which can be directly coupled to the antibody following reduction and alkylation in a single step. The product is then purified to remove any unreacted drugs.
Kit is designed to conjugate 1-3 mg of a single antibody sample (CM11431x1) or three antibody samples (CM11431x3).
If you have a smaller amount of IgG, a non-IgG type antibody, or other customization needs, please select the customization radio button and/or fill out the information above.
Antibody Loading
Due to the unknown characteristics of many customers’ antibodies, this kit is designed to attach an average of 4 molecules of deruxtecan to each antibody molecule. Trastuzumab Deruxtecan, sold under the brand name Enhertu, has an average of 8 deruxtecan molecules attached per antibody. If your target is 8 and you have not observed significant aggregation or precipitation with your antibody using this kit, you can go ahead and use CM11434 (Antibody Deruxtecan High Loading Conjugation Kit) for higher loading.
Drug Information
- 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 Antibody
- Preferably >90% pure by gel electrophoresis
- Total amount: 1-3 mg of protein content as measured by UV.
Key Features of this PerKit™
- Simple and efficient labeling of IgG with Deruxtecan, minimizing toxin exposure.
- Features enzymatic cleavable GGFG peptide linker.
- Delivers an average of 4 Deruxtecan molecules per antibody.
- Fast preparation: 4 hours total, with less than 1 hour of hands-on time.
- Includes all necessary reagents and supplies for preparation and purification.
- Achieves over 95% conjugation, free from unreacted drugs.
- Post-conjugation services are available from CellMosaic for analysis and DAR determination.
Conjugation Chemistry
Protocol
Schematic workflow diagram for preparing antibody-Deruxtecan conjugates, starting with 3 mg of IgG. (Reagent volumes will vary if the amount of IgG is less than 3 mg.)
Related Products
ADC Control hIgG1-Deruxtecan (Product #: CM51103): A control ADC made with a non-binding human IgG1 subtype. This product contains an average of 4 deruxtecan molecules per antibody and has low endotoxin levels, making it suitable for in vitro and in vivo studies.
ADC Control Kit with VC-PAB Linker (Product #: CM11429): A negative control ADC preparation kit utilizing the VC-PAB linker.
Hydrophobic Interaction Chromatography (HIC) Buffer Set (Product#: CM02025): Designed for ADCs prepared via reduced thiols of the antibody, HIC HPLC is used to calculate the Drug-to-Antibody (DAR) and assess ADC heterogeneity. Conjugates are separated based on hydrophobicity, and antibodies with the same DAR will elute as a single peak. For typical MMAE ADCs, multiple peaks represent varying drug loads. The HIC Buffer set is accompanied by a product sheet with all of the information and methodology needed for HIC HPLC analysis. If you lack HPLC access, CellMosaic® offers sample analysis services.
Size Exclusion Chromatography (SEC) HPLC Protein Standards (Product #: CM92004 and CM92005): SEC HPLC separates the conjugates by apparent molecular weight (MW) or size in an aqueous solution. Larger MW conjugates elute earlier. Comparing SEC profiles of unlabeled IgG and ADCs allows you to estimate aggregation levels. CellMosaic® provides two SEC standards for use with any SEC column. The product sheet includes detalied methodology for running SEC HPLC analysis. If you lack HPLC access, CellMosaic® can perform the analysis for you.
ADC stabilizing PBS buffer (5x) (Product #: CM02022): This buffer contains 5x PBS and other stabilizers to prevent hydrophobic drug interactions during storage, which can cause ADC precipitation. It also preserves ADC structure lyophilization. The buffer is biocompatible and suitable for in vitro and in vivo studies.
