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.

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.

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.

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.

PNU-EDA is a part of the antibody-conjugated active molecule ADC. It is formed by coupling a cleavable ADC linker (EDA) with the payload PNU159682. PNU-EDA can be used for the synthesis of ADC compounds.

C-lock-GGFG-DXd is a thiol-reactive drug linker. GGFG is an enzyme-degradable peptide. After entering the lesion site, it can release the payload DXd and exert its function. C-lock-GGFG-DXd is commonly used in the synthesis of antibody-drug conjugates (ADCs).

C-lock-GGFG-Exatecan is a thiol-reactive drug linker. GGFG is a peptidase-activatable peptide. After entering the lesion, it can enable the release and activation of the payload Exatecan. C-lock-GGFG-Exatecan is commonly used in the synthesis of antibody-drug conjugates (ADCs).

MC-VC-PAB-Exatecan is a part of the antibody-conjugated active molecule ADC. It is formed by coupling the cleavable ADC linker (MC-VC-PAB) with the payload Exatecan. MC-VC-PAB-Exatecan is commonly used in the synthesis of ADC compounds.

Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27) is an active molecular conjugate used in antibody-drug conjugates (ADCs), consisting of the ADC linker Mal-N(Me)-C6-N(Me) and the potent cytotoxin PNU-159682. This compound selectively delivers its payload to cells expressing CD46 and releases PNU-159682 through cathepsin B cleavage of the linker, inducing DNA damage and apoptosis. Mal-N(Me)-C6-N(Me)-PNU-159682 has demonstrated sustained tumor regression in patient-derived xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal cancer (CRC).