A desirable monoclonal antibody, an effective cytotoxic drug, and a suitable linker make up antibody-drug conjugates (ADCs). A suitable linker between the antibody and the cytotoxic drug creates a clear bridge, enabling the antibody to precisely deliver the cytotoxic drug to tumor sites and deliver it only to tumor cells. In addition to conjugation, the linkers preserve the stability of ADCs during their preparation, storage, and systemic circulation phases.
The linkers found in the ADCs currently undergoing clinical evaluation are primarily divided into two groups: cleavable and noncleavable. Cleavable linkers rely on internal cellular mechanisms to release the toxin, such as cytoplasmic reduction, exposure to acidic conditions in the lysosome, or cleavage by particular cellular proteases. For the release of the cytotoxic molecule with noncleavable linkers, the antibody portion of the ADC must be broken down by proteolytic enzymes while retaining the linker and the amino acid by which it was attached to the antibody.
Based on knowledge of the internalization and breakdown of the antibody-target antigen complex and a comparison of the preclinical in vitro and in vivo activities of conjugates, the choice of linker depends on the target. Additionally, because each molecule has different chemical restrictions and frequently the drug structure lends itself to a particular linker, the choice of a linker is also influenced by the type of cytotoxin used.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V76105 | Tetra-O-acetyl-β-D-galactopyranosyl-Ph-CH2-(4-nitrophenyl)carbonate-Fmoc | 2169723-91-3 | Tetra-O-acetyl-β-D-galactopyranosyl-Ph-CH2-(4-nitrophenyl)carbonate-Fmoc (Example 2.28.6) is an ADC linker that may be utilized to prepare Antibody-drug conjugates (ADC). |
|
V52570 | Tetrazine-PEG4-amine hydrochloride | 2752945-36-9 | Tetrazine-PEG4-amine ( HCl) is a cleavable ADC (Antibody-drug conjugate) linker containing 4 PEG (polyethylene glycol) units, which may be utilized to prepare active ADC molecules. |
|
V76441 | Tetrazine-PEG7-amine hydrochloride | Tetrazine-PEG7-amine HCl is a cleavable ADC (Antibody-drug conjugate) linker containing 7 PEG (polyethylene glycol) units, which may be utilized to prepare active ADC molecules. | |
|
V54607 | trans-Sulfo-SMCC | 1286837-77-1 | trans-Sulfo-SMCC is a non-cleavable (non-degradable), membrane-permeable/penetrable ADC cross-linker. |
|
V54661 | Trisulfo-Cy3 Methyltetrazine | 1676067-48-3 | Trisulfo-Cy3 Methyltetrazine is a reagent for click chemistry containing a methyltetrazine group. |
|
V54604 | Tup hydrochloride | 1200041-11-7 | Tup HCl is a cleavable (degradable) ADC (Antibody-drug conjugate) linker. |
|
V88366 | Val-Ala-PAB | 1343476-44-7 | Val-Ala-PAB is a cleavable ADC linker that can be used in the synthesis of ADCs. |
|
V103535 | Val-Cit-PAB-DEA-COOH | 2270986-50-8 | Val-Cit-PAB-DEA-COOH (Compound 17) is an ADC linker that can be used in the synthesis of ADCs. |
|
V54669 | Val-Cit-PAB-OSBT | 2210262-26-1 | Val-Cit-PAB-OSBT GMP is GMP grade Val-Cit-PAB-OSBT. |
|
V54541 | Val-Cit-PABC-Ahx-May | 2126749-74-2 | Val-Cit-PABC-Ahx-May is a cleavable (degradable) ADC (Antibody-drug conjugate) linker that may be utilized to prepare active antibody conjugated molecules (ADC). |
|
V54534 | Val-Cit-PABC-Ahx-May TFA | 2126749-75-3 | Val-Cit-PABC-Ahx-May TFA is a cleavable (degradable) ADC (Antibody-drug conjugate) linker that may be utilized to prepare antibody-conjugated active molecules (ADC). |
|
V2314 | Val-Lys(Boc)-PAB | 1432969-86-2 | PAB-Val-Lys-Boc is a cleavable (degradable) ADC (Antibody-drug conjugate) linker that may be utilized to prepare antibody-conjugated active molecules (ADC) to stimulate immune responses. |
|
V54507 | vc-PABC-DM1 | 1416792-90-9 | vc-PABC-DM1 is used to synthesize disulfide linker-based ADC molecules. |
|
V54495 | XMT-1519 conjugate-1 | 2720500-19-4 | ΧΜT-1519 conjugate-1 (compound 31) is a linker of the HER-2 monoclonal antibody (mAb) XMT-1519, which may be utilized to prepare ADC and increase anti-tumor activity. |
|
V76133 | Z-AEVD-FMK | 1135688-47-9 | Z-AEVD-FMK is a cleavable (degradable) ADC (Antibody-drug conjugate) linker used for the synthesis of antibody active molecule conjugates (ADCs). |
|
V54707 | ZD-Dbu(N3)-OH | 1931958-82-5 | ZD-Dbu(N3)-OH is a reagent for click chemistry containing an Azide (N3) moiety. |
|
V54605 | ZL-Aha-OH | 1263047-43-3 | ZL-Aha-OH is a reagent for click chemistry containing an Azide (N3) moiety. |
|
V54542 | ZL-Aha-OH (DCHA) | 1423018-09-0 | ZL-Aha-OH (DCHA) is an Azide (N3) moiety-containing click chemistry reagent. |
|
V54723 | ZL-Dap(N3)-OH | 684270-44-8 | ZL-Dap(N3)-OH is a reagent for click chemistry bearing an azide (N3) moiety. |
|
V54662 | ZL-Dbu(N3)-OH | 1932657-23-2 | ZL-Dbu(N3)-OH is a dot chemical reagent containing azide. |
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