linker-payload

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.

Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50 = 650 nM). It inhibits multiple cancer cell lines via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome, displaying low-nM to sub-nM IC50s. Thailanstatin A, as a payload for ADCs, is conjugated to the lysines on trastuzumab, yielding linker-less ADC.

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.

Rinatabart sesutecan is a highly homogeneous antibody-drug conjugate (ADC) targeting folate receptor alpha (FRα). Rinatabart sesutecan consists of a humanized antibody targeting FRα, a hydrophilic cleavable linker, and the topoisomerase I inhibitor exatecan as the payload. It is primarily used for the targeted treatment and mechanistic research of folate receptor-positive solid tumors.

ABBV-706 is an antibody-drug conjugate (ADC) that targets the receptor tyrosine kinase SEZ6. After binding to the surface of tumor cells, it is internalized and releases a cytotoxic payload, thereby inducing tumor cell death. ABBV-706 is currently in clinical development and has demonstrated potential antitumor activity in solid tumors such as small cell lung cancer.

m-PEG4-Br is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADC) for Trastuzumab, positioned distally from the monomethyl auristatin E (MMAE) payload to produce an ADC with modified hydrophilicity, antigen binding, and in vitro potency[1].

DBCO-(PEG2-VC-PAB-MMAE)2 consists of Monomethyl auristatin E (MMAE), a potent tubulin inhibitor and toxin payload in antibody-drug conjugate [1], conjugated to the cleavable linker DBCO-(PEG2-VC-PAB)2, serving as the cytotoxic component in this formulation.

DBCO-PEG4-SS-TCO is a cleavable 4-unit polyethylene glycol (PEG) linker crucial for the synthesis of antibody-drug conjugates (ADCs)[1], facilitating the connection of the drug payload to the antibody and enabling targeted drug delivery.

DBCO-(PEG)3-VC-PAB-MMAE is a chemical compound where monomethyl auristatin E (MMAE), a potent tubulin inhibitor used as a toxin payload in antibody-drug conjugates, is conjugated via a DBCO-(PEG)3-vc-PAB linker.

Gly-Gly-Gly-PEG4-methyltetrazine is a cleavable four-unit PEG-based antibody–drug conjugate (ADC) linker that is specifically engineered to facilitate efficient conjugation and controlled payload release,Gly-Gly-Gly-PEG4-methyltetrazine is widely utilized in the synthesis and optimization of ADCs, enabling precise bioconjugation, improved pharmacokinetic performance, and enhanced therapeutic index in targeted drug delivery research.

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-Phe-C4-VC-PAB-MMAE is a chemical compound formed by conjugating monomethyl auristatin E (MMAE), a potent tubulin inhibitor used as a toxin payload in antibody-drug conjugates, with a Mal-Phe-C4-VC-PAB linker.

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.

Vc-seco-DUBA (Duocarmazine) is a linker-payload conjugate designed for the synthesis of Antibody-Drug Conjugates (ADCs). It consists of the potent DNA alkylating payload DUBA (a duocarmycin analog) connected via the Vc-seco linker. This conjugate is engineered to enable the targeted delivery of highly cytotoxic DNA-alkylating agents specifically to tumor cells through antibody guidance. DUBA exerts its effect by binding to the minor groove of DNA and causing alkylation, which leads to DNA damage and subsequent apoptosis, demonstrating potent antitumor efficacy.

NAMPT inhibitor-linker 1, a drug-linker conjugate for ADC, integrates an NAMPT inhibitor (as a payload) with a linker. In the formulation of ADC-3, it pairs with an anti-c-Kit monoclonal antibody, demonstrating strong efficacy against c-Kit expressing cell lines, specifically GIST-T1 and NCI-H526, where it exhibits IC50 values of <3 pM and 9 pM, respectively.

NAMPT inhibitor-linker 2, a drug-linker conjugate for antibody-drug conjugates (ADCs), comprises an NAMPT inhibitor payload and a linker. When combined with an anti-c-Kit monoclonal antibody to form ADC-4, it demonstrates potent efficacy against c-Kit expressing cell lines, including GIST-T1 and NCI-H526, with IC50 values of <7 pM and 40 pM, respectively.

PC Mal-NHS carbonate ester is a cleavable linker specifically designed for the synthesis of antibody-drug conjugates (ADCs)[1]. This chemical compound facilitates drug-antibody conjugation, enabling targeted delivery and enhanced therapeutic efficacy. Its unique carbonate ester structure allows efficient cleavage in the targeted environment, ensuring controlled drug payload release, highlighting its significance in innovative and targeted cancer therapies.

SPDB-DM4 is a drug-linker conjugate designed for antibody-drug conjugate (ADC) applications, employing the maytansine-based payload DM4 (a tubulin inhibitor) connected through a SPDB linker. This compound demonstrates significant anti-tumor efficacy.

Sulfo-SPDB-DM4 is a drug-linker conjugate designed for antibody-drug conjugates (ADCs) that employs the maytansine-based payload (DM4, an antitubulin agent) connected through the sulfo-SPDB linker.

Mal-Toxophore is a drug-linker complex used in the synthesis of ADCs (Antibody-Drug Conjugates). Its active payload consists of an NAMPT inhibitor.

APL-1092 (Mal-Exo-EEVC-Exatecan) is a drug-linker conjugate utilized in the synthesis of antibody-drug conjugates (ADCs), comprising Exatecan (ADC payload) and a linker within its structure.

Mal-PEG4-Val-Cit-PAB-MMAE is the linker-payload component of an antibody-conjugated active molecule (ADC), consisting of a degradable ADC linker and the microtubule inhibitor MMAE.

MC-Val-Cit-PAB-Sunitinib is a conjugate composed of the payload Sunitinib and a linker. It is utilized in the synthesis of HR97-Sunitinib.

CTT2274 is a prodrug of MMAE. It consists of a prostate-specific membrane antigen (PSMA) binding scaffold, a biphenyl motif, a pH-sensitive phosphoramidate linker, and an MMAE payload. CTT2274 selectively targets and binds to PSMA to deliver MMAE and has the capability to inhibit prostate cancer.