drug-linker conjugates for adc

Deruxtecan is an ADC drug-linker conjugate composed of a derivative of DX-8951 (DXd) and a maleimide-GGFG peptide linker used in the synthesis of DS-8201 and U3-1402.

Lys-SMCC-DM1 (Lys-Nε-MCC-DM1) is an antibody-drug conjugate (ADC) targeting human epidermal growth factor receptor 2 (HER2). It contains the microtubule polymerization inhibitor DM1 as the active metabolite, which inhibits microtubule polymerization. It is commonly used in breast cancer research.

McMMAF is a protective group-conjugated MMAF. MMAF is a potent tubulin polymerization inhibitor.It is a MMAF derivative having a Maleimidocaproyl linker (MC linker), which is ready to conjugate to antibody or other proteins or biopolymers. Mafodotin is a useful agent for make antibody drug conjugate (ADC) for targeted drug delivery.

SMCC-DM1 is a drug-coupler coupler consisting of a potent microtubule disrupter, DM1, and a coupler, SMCC, for the preparation of antibody-drug couplers.

CL2A-SN-38 consists of a CL2A linker and an anticancer compound, SN-38, which delivers active molecules within tumor cells and in the tumor microenvironment, often in conjunction with antibodies to make biologically active antibody-coupled reactive molecules (ADCs).

Fmoc-Val-Cit-PAB-MMAE is consisted of the ADCs linker (Fmoc-Val-Cit-PAB) and potent tubulin inhibitor (MMAE). Fmoc-Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC.

Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) is a drug-linker conjugate for ADC. Mc-MMAE is a maleimidocaproyl-conjugated monomethyl auristatin E, which is a potent tubulin inhibitor.

Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC. Val-Cit-PAB-MMAE contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin inhibitor MMAE . MMAE a potent mitotic inhibitor by inhibiting tubulin polymerization[1].

Vc-MMAD, a drug-linker conjugate for Antibody-Drug Conjugates (ADCs), combines the ADC linker Val-Cit (Valine-Citrulline) with the potent tubulin inhibitor MMAD. This compound leverages the targeting capability of ADCs to deliver the cytotoxic agent MMAD specifically to cancer cells, enhancing therapeutic efficacy while minimizing off-target effects.

PSMA-ALB-56 is a PSMA-targeting radioactive ligand with antitumor activity, composed of glutamic urea PSMA binding entities, DOTA chelating agents, and albumin binders based on 4-(p-iodophenyl)- fragment or p(tolyl)- fragment.

VCMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate for ADC with potent antitumor activity.

ABBV-969 Payload (Br-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT) is a drug-linker conjugate employed in the synthesis of antibody-drug conjugates (ADCs). The ABBV-969 Payload contains a Topoisomerase I inhibitor molecule and a chemical linker, enabling coupling with anti-c-Met antibodies to generate ABBV-969 ADCs with targeted anticancer activity.

Acetylene-linker-Val-Cit-PABC-MMAE (LCB14-0602) is a drug-linker conjugate for antibody-drug conjugates (ADCs), combining the ADC linker (Acetylene-linker-Val-Cit-PABC) with the potent tubulin inhibitor MMAE.

DBCO-PEG4-VC-PAB-DMEA-PNU-159682, a drug-linker conjugate for antibody-drug conjugates (ADC), comprises the ADC linker DBCO-PEG4-VC-PAB and the potent ADC cytotoxin DMEA-PNU-159682, which includes metabolites of nemorubicin (MMDX) from liver microsomes and the ADC cytotoxin PNU-159682[1].

DM4-SMCC, a non-cleavable drug-linker conjugate for antibody-drug conjugates (ADC), leverages the antitumor efficacy of DM4 (an antitubulin agent) through attachment with the SMCC linker, exhibiting antitumor activity[1].

Gemcitabine-O-Si(di-iso)-O-Mc, a drug-linker conjugate for Antibody-Drug Conjugates (ADC), exhibits potent antitumor activity. It incorporates Gemcitabine, a pyrimidine nucleoside analog antimetabolite and antineoplastic agent, connected through the ADC linker [1].

Mal-C2-Gly3-EDA-PNU-159682, a drug-linker conjugate for antibody-drug conjugates (ADC), integrates the cleavable ADC linker Mal-C2-Gly3-EDA with the potent cytotoxin PNU-159682.

Mal-PEG2-VCP-Eribulin is a chemotherapeutic compound comprising an antibody-drug conjugate (ADC) linker (Mal-PEG2-VCP) and the microtubule inhibitor Eribulin[1]. This compound uniquely targets microtubules, offering a novel approach to cancer treatment. Eribulin is specifically utilized in creating targeted Eribulin-based drugs for antibody conjugates[1].

Mal-PEG4-VA-PBD is a commonly used linker-toxin conjugate structure in antibody-drug conjugates (ADCs). It consists of Mal for conjugation to antibody thiols, PEG4 as a hydrophilic spacer arm to improve solubility, VA as a dipeptide linker cleavable by lysosomal proteases, and a pyrrolobenzodiazepine (PBD) DNA alkylator as the cytotoxic payload. Mal-PEG4-VA-PBD is cleaved by proteases upon cell entry to release PBD, which then forms covalent adducts with DNA and induces cell death.

Mal-VC-PAB-DM1, a drug-linker conjugate for antibody-drug conjugates (ADCs), exhibits potent antitumor activity. It incorporates DM1, a potent microtubule-disrupting agent, connected through the ADC linker Mal-VC-PAB [1].

Mc-MMAD is monomethyl auristatin D (MMAD) modified with the protective group maleimidocaproyl (Mc). MMAD is a potent tubulin microtubule inhibitor that suppresses cancer cell proliferation and is commonly employed as a toxic payload in ADC synthesis.

MC-Sq-Cit-PAB-Dolastatin10 is a potent antitumor drug-linker conjugate for Antibody-Drug Conjugates (ADC), incorporating Dolastatin10 (a tubulin polymerization inhibitor) connected via the MC-Sq-Cit-PAB ADC linker.

MC-Sq-Cit-PAB-Gefitinib is a potent antitumor drug-linker conjugate for Antibody-Drug Conjugates (ADC), utilizing Gefitinib—an EGFR tyrosine kinase inhibitor—connected through the MC-Sq-Cit-PAB ADC linker.

MC-Val-Cit-PAB-carfilzomib is a potent antitumor drug-linker conjugate for antibody-drug conjugates (ADC), comprising the irreversible proteasome inhibitor carfilzomib, connected through the ADC linker MC-Val-Cit-PAB.