Drug conjugates have attracted widespread attention for their clinical outcomes and potential commercial value. A variety of drug conjugates have been developed including antibody-drug conjugates (ADCs), peptide-drug conjugates (PDCs), antibody-oligonucleotide conjugates (AOCs), radionuclide-drug conjugates (RDCs), antibody fragment-drug conjugates (FDCs), aptamer-drug conjugates (ApDCs), small molecule-drug conjugates (SMDCs), etc. These therapeutic conjugates are generated through covalent conjugation of therapeutic molecules to antibody, peptide, radionuclide, antibody fragment, aptamer, or small molecular ligands via linkers.
Amerigo Scientific offers PerKits™ drug conjugation kits to rapidly evaluate the biologics of interest (such as antibodies, proteins, peptides, and oligos) with direct conjugations of a range of key payloads (chemotherapeutic drugs and toxins) and traditional linker chemistry. PerKits™ kits are available in a variety of configurations and conjugation strategies. Some PerKits™ drug conjugation kits are suitable for general payloads with specific functional groups such as carboxylic acids and amines. Some PerKits™ kits provide selected, standard linker molecules conjugated to selected payloads, which are ready with appropriate reactive modifications, to enable direct attachment of the payloads and linkers to the specific biologics of interest.
PerKits™ kits contain the full set of reagents required to allow the selected payload to directly attach to the biomolecule of interest and purify the final drug conjugate. The only additional items the client needs to provide are the biologics of interest and general laboratory equipment.
PerKits™ ADC Conjugation Kits | PerKits™ PDC Conjugation Kits |
PerKits™ FDC Conjugation Kits | PerKits™ Oligo Conjugation Kits |
ADCs are a promising cancer therapy modality that can selectively deliver cytotoxic payloads to target cells. Comprised of a monoclonal antibody conjugated to a cytotoxic payload, the ADC combines the selectivity of the antibody with the cell killing power of the payload. Amerigo Scientific offers PerKits™ conjugation kits for the preparation of ADCs and some of these ADCs can be stored at 4°C for a few weeks or months.
PerKits™ ADC kits can be used to prepare approximately 2-3 mg of final ADCs in a buffer with average drug-antibody ratios (DARs) of 2-4. The purity of the final ADCs is usually greater than 90%, and the unreacted payload is less than 5%. The results may vary depending on the specific antibody system used and the hydrophobicity of the payload. Our kits are easy to operate and conjugation can typically be performed within 6 hours.
Product | Biomolecule | Drug | Scale of Reaction (Standard Kit) | Labeling Chemistry | Linkage |
---|---|---|---|---|---|
ADC Control Kit with VC-PAB Linker | IgG Ab | No drug (VC-PAB linker only) |
1-3 mg | Reduced thiol | Releasable |
PerKit™ Antibody Small Molecule Acid Conjugation Kit | IgG Ab | Acid | 1-3 mg | Surface amine | Stable |
Antibody Mertansine (DM1) Conjugation Kit | IgG Ab | Mertansine (DM1) | 0.1 mg, 1-3 mg | Surface amine | Stable |
Antibody Doxorubicin Conjugation Kit | IgG Ab | Doxorubicin | 1-3 mg | Surface amine | Stable |
Antibody Methotrexate Conjugation Kit | IgG Ab | Methotrexate | 1-3 mg | Surface amine | Stable |
Antibody MMAE Conjugation Kit (With VC-PAB Linkage) | IgG Ab | MMAE | 0.1 mg, 1-3 mg | Reduced thiol | Releasable |
Antibody Mc-MMAF Conjugation Kit | IgG Ab | MMAF | 1-3 mg | Reduced thiol | Stable |
Antibody MMAF Conjugation Kit (with VC-PAB Linker) | IgG Ab | MMAF | 1-3 mg | Reduced thiol | Releasable |
Antibody SN38 Conjugation Kit | IgG Ab | 7-ethyl-10-hydroxycamptothecin (SN38) | 1-3 mg | Surface amine | Releasable |
Antibody Deruxtecan Conjugation Kit | IgG Ab | Deruxtecan | 1-3 mg | Reduced thiol | Releasable |
F(ab')2 MMAE Conjugation Kit (With VC-PAB Linkage) | F(ab')2 | MMAE | 0.73-2.2 mg | Reduced thiol | Releasable |
F(ab')2 Mertansine (DM1) Conjugation Kit | F(ab')2 | Mertansine (DM1) | 0.73-2.2 mg | Surface amine | Stable |
Amerigo Scientific offers PerKit™ kits for peptide labeling and conjugation, which are suitable for the peptides easily synthesized with 5’ or 3’ Cys modification. PerKits™ PDC kits are available for the preparation of approximately 50 nmol of final PDC in buffer with DARs of 2 to 5 (average DAR values of 3-4). The purity of the final conjugate is great than 90%, and the free payload is less than 5%. The results may vary depending on the specific protein system used and the hydrophobicity of the payload. PerKits™ PDC kits are easy to operate and the conjugation can typically be carried out within 4 hours.
Product | Biomolecule | Drug | Scale of Reaction (Standard Kit) | Labeling Chemistry | Linkage |
---|---|---|---|---|---|
PerKit™ Protein Small Molecule Acid Conjugation Kit | Any protein | Acid | 15-50 nmol | Surface amine | Stable |
Protein Mertansine (DM1) Conjugation Kit | Any protein | DM1 | 6.67-20 nmol | Surface amine | Stable |
Protein SN38 Conjugation Kit | Any protein | SN38 | 6.67-20 nmol | Surface amine | Releasable |
Protein MMAE Conjugation Kit | Any protein | MMAE | 6.67-20 nmol | Surface amine | Releasable |
Protein Deruxtecan Conjugation Kit | Any protein | Deruxtecan | 6.67-20 nmol | Surface amine | Releasable |
Antibody fragment-drug conjugates (FDCs) are the specific, low-immunity and small-size antibody fragments conjugated to cytotoxic payloads. Compared with ADCs, FDCs are smaller in molecular size and thus have better diffuse penetration ability into tissues. FDCs can improve the delivery rate of cytotoxic agents and increase the accumulation in the target tissues. Amerigo Scientific offers PerKits™ conjugation kits for coupling any F(ab')2 with a cytotoxic agent using VC-PAB or SMCC linker.
Product | Biomolecule | Drug | Scale of Reaction (Standard Kit) | Labeling Chemistry | Linkage |
---|---|---|---|---|---|
F(ab')2 MMAE Conjugation Kit (With VC-PAB Linkage) | F(ab')2 | MMAE | 0.73-2.2 mg | Surface amine | Stable |
F(ab')2 Mertansine (DM1) Conjugation Kit | F(ab')2 | DM1 | 0.73-2.2 mg | Reduced thiol | Releasable |
Amerigo Scientific offers PerKits™ conjugation kits for oligonucleotide conjugation, which are suitable for oligonucleotides with 5’ or 3’ amine or thiol modifications.
Product | Scale of Reaction | Labeling Chemistry | Linkage |
---|---|---|---|
AP Oligo Conjugation Kit (Single Label with Amine Oligo) | 2.5 nmol oligo | Amine oligo | Stable |
HRP Oligo Conjugation Kit (Single Label with Amine Oligo) (Replacement) | 1-5 nmol oligo | Amine oligo | Stable |
HRP Oligo Conjugation Kit (Single Label with Thiol Oligo) (Replacement) | 2-5 nmol oligo | Thiol oligo | Stable |
Streptavidin Oligo Conjugation Kit (Single Label with Amine Oligo) | 2-5 nmol oligo | Amine oligo | Stable |
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