Drug-Linker Conjugates for ADC

SMCC-DM1 (DM1-SMCC) (DM1-SMCC) is a drug-linker conjugate which composed of a potent microtubule-disrupting agent DM1 and a linker SMCC to make antibody-drug conjugate (ADC).

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

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.

Deruxtecan (1R) is a drug-linker conjugate for antibody-drug conjugates (ADC) [1].

MC-DM1 is a drug-linker conjugate composed of a potent microtubule-disrupting agent DM1 and a linker MC to make antibody drug conjugate (ADC).

MC-SN38 is a drug-linker conjugate that pairs the potent microtubule-disrupting agent SN38 with a non-cleavable MC linker, designed for use in antibody drug conjugates (ADCs). SN38, the active metabolite of the Topoisomerase I inhibitor Irinotecan, works by inhibiting DNA synthesis and inducing DNA single-strand breaks.

Biotin-PEG7-Maleimide is a biotinylation agent that selectively binds to thiol (SH) groups and is utilized in the synthesis of Drug-Linker Conjugates for Antibody-Drug Conjugates (ADCs) [1].

DGN549-L is a DNA alkylator that facilitates antibody conjugation at lysine residues, making it suitable for antibody-drug conjugate (ADC) synthesis.

AcLys-PABC-VC-Aur0101 is a drug-linker conjugate for anti-CXCR4 ADC with potent antitumor activity, comprising the auristatin microtubule inhibitor Aur0101, connected through the cleavable linker AcLys-PABC-VC[1].

SuO-Glu-Val-Cit-PAB-MMAE is a chemical compound comprising a cleavable ADC linker, SuO-Glu-Val-Cit-PAB, and a potent tubulin inhibitor known as MMAE. It is utilized in the synthesis of antibody-drug conjugates (ADCs).

MC-VC-PABC-Aur0101 is a potent anticancer drug-linker conjugate designed for Antibody-Drug Conjugates (ADCs), comprising Aur0101, an auristatin microtubule inhibitor, connected through the MC-VC-PABC linker to enhance antitumor efficacy.

Mal-C6-α-Amanitin, an ADC (antibody-drug conjugate) linker drug, incorporates the powerful antitumor agent α-Amanitin, an inhibitor of RNA polymerase II, through the Mal-C6 linker, showcasing potent antitumor activity.

MC-Alkyl-Hydrazine Modified MMAF is a potent antitumor drug-linker conjugate for ADC, incorporating Modified MMAF, a tubulin inhibitor, through a noncleavable MC-Alkyl-Hydrazine linkage[1].

DBCO-PEG4-VA-PBD is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

ST8155AA1, a component of antibody-drug conjugates (ADCs), is tethered to an HDAC inhibitor via a linker and exhibits antitumor activity [1].

SMP-33693 is an Antibody-Drug Conjugate (ADC) known for its low payload shedding rate and demonstrated in vivo tumor inhibition in ovarian, gastric, and breast cancers [1].

MC-VC-PABC-C6-alpha-Amanitin is an antibody-drug conjugate that combines the anticancer toxin alpha-Amanitin with the monoclonal antibody MC-VC-PABC-C6. Alpha-Amanitin acts as a potent inhibitor of RNA polymerase IIα, enabling the conjugate to selectively target and recognize HER2-positive tumor cells. This specificity makes MC-VC-PABC-C6-alpha-Amanitin a valuable research tool in the study of breast and gastric cancers [1].

MC-GGFG-(7ethanol-10NH2-11F-Camptothecin) (compound 141) is a protease-cleavable drug-linker conjugate utilized in antibody-drug conjugates (ADCs), featuring an MC-GGFG linker that allows for enzymatic cleavage [1].

Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan is a linker molecule employed in the synthesis of antibody-drug conjugates (ADCs), demonstrating potent antitumor activity both in vitro and in vivo [1].

Gly-Mal-Gly-Gly-Phe-Gly-amide-methylcyclopropane-Exatecan is a compound utilized in the synthesis of Antibody-Drug Conjugates (ADCs) [1].

Vc-seco-DUBA is a drug-linker conjugate for ADC with potent antitumor activity by using DUBA (DNA alkylating agent), linked via the ADC linker Vc-seco[1].

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.

Aminobenzenesulfonic Auristatin E TFA, an agent-linker conjugate for ADC, exhibits potent antitumor activity. It employs Auristatin E (a cytotoxic tubulin modifier) connected through the ADC linker Aminobenzenesulfonic [1].

Mipsagargin (G-202) is a new antibiotic that inhibits DNA biosynthesis.

Desmethyl Vc-seco-DUBA, a compound comprising a cleavable ADC linker (Desmethyl Vc-seco) and a DNA alkylating agent (DUBA), is utilized in the synthesis of antibody-drug conjugates (ADCs) [1].

MP-PEG8-VA-PABC-PBD Dimer is a drug-linker conjugates for ADC which is used in the treatment of several cancers. PBD Dimer is a DNA alkylating which inhibits DNA replication[1].

Amino-PEG4-Val-Cit-PAB-MMAE is a cleavable tetraethylene glycol (4 unit PEG) antibody-drug conjugate (ADC) linker employed in the synthesis of ADCs[1].

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].

Doxorubicin-SMCC is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

MC-vc-PAB-Tubulysin M is a conjugate composed of a cleavable ADC linker (MC-vc-PAB) and the cytotoxic tubulin inhibitor Tubulysin M, which inhibits tubulin polymerization, resulting in cell cycle arrest and apoptosis.

CL2-SN-38, a part of the antibody-drug conjugate (ADC), can conjugate with the anti-Trop-2-humanized antibody hRS7. SN-38 is an inhibitor of DNA topoisomerase I.

MAL-di-EG-Val-Cit-PAB-MMAF refers to a chemical compound that comprises the linker (MAL-di-EG-Val-Cit-PAB) and the potent blocker of tubulin polymerization (MMAF, Monomethyl auristatin F)[1].

Val-Cit-PAB-MMAE is a molecular entity designed to function as an antibody-drug conjugate (ADC) or as a component of bispecific antigen-binding molecules, specifically targeting the hepatocyte growth factor receptor known as c-Met (MET).

TLR7/8 agonist 4 hydroxy-PEG6-acid, a Drug-Linker Conjugate for ADCs, comprises the TLR7/8 agonist 4 and a hydroxy-PEG6-acid linker, suitable for the synthesis of antibody-drug conjugates (ADCs) [1].

SN38-PAB-Lys(MMT)-oxydiacetamide-PEG8-N3 is a drug-linker conjugate for antibody-drug conjugates (ADCs), consisting of the anti-cancer agent SN38 linked to Lys(MMT)-PAB-oxydiacetamide-PEG8-N3. It serves as a click chemistry reagent featuring an azide group that participates in copper-catalyzed azide-alkyne cycloaddition (CuAAC) with alkyne-bearing molecules and can also engage in strain-promoted alkyne-azide cycloaddition (SPAAC) with compounds containing DBCO or BCN groups, facilitating the synthesis of ADCs [1].

PSMA-Val-Cit-PAB-MMAE is a novel PSMA-targeted small-molecule conjugate leveraging monomethyl auristatin E (MMAE) for prostate cancer chemotherapy.

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

Mal-Phe-C4-VC-PAB-MMAE is a chemical compound resulting from the conjugation of monomethyl auristatin E (MMAE), a potent tubulin inhibitor serving as a toxin payload in antibody-drug conjugates, with a Mal-Phe-C4-VC-PAB linker.

Mal-VC-PAB-PNP-CDN-A is a conjugate comprised of an agent and a linker, utilized in antibody-drug conjugates (ADC) [1] [2].

Compound 15, Mal-PEG8-Phe-Lys-PAB-Exatecan, is an antibody-drug conjugate (ADC) comprised of the degradable linker Mal-PEG8-Phe-Lys-PAB and the cytotoxic agent Exatecan [1].

HS-(CH2)3CO-L-Ala-D-Ala-L-Ala-NH-CH2-S-(CH2)5-CO-DM is a peptide-cleavable agent-linker conjugate utilized in antibody-drug conjugates (ADCs), with the DM denoting the maytansinoid component [1].

Compound 10, Aminooxy CatB-LXR, constitutes an agent-linker conjugate for antibody-drug conjugates (ADC) [1].

Amidate-VC-PAB-MMAF, a cleavable ADC linker (Amidate-VC-PAB) combined with a potent tubulin polymerization inhibitor (MMAF), is utilized in the synthesis of antibody-drug conjugates (ADCs) to decrease off-target cytotoxicity[1].

PNU-EDA-Gly5 is a DNA topoisomerase I inhibitor-based oligo-glycine linker-payload used for the synthesis of antibody-drug conjugates (ADCs). It consists of the DNA topoisomerase I inhibitor PNU-159682 and the linker EDA-Gly5.

MCC-DM1 is a drug-Linker Conjugates for ADC such ad Anti-CD22-MCC-DM1.

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

MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan is an agent-linker conjugate for antibody-drug conjugates (ADCs), incorporating Exatecan, a DNA Topoisomerase I inhibitor (IC 50 = 2.2 μM) [1].

Fmoc-VAP-MMAE is a conjugate utilized in antibody-drug conjugates (ADCs), comprising a tubulin inhibitor, monomethyl auristatin E (MMAE), connected via an ADC linker, and shielded by a fluorenylmethyloxycarbonyl (Fmoc) protective group [1].

CL2E-SN-38 is a structurally stable and highly releasable antibody-drug conjugate (ADC) incorporating SN-38, the active metabolite of Irinotecan and a potent Topoisomerase I inhibitor [1] from the camptothecins class.

DBA-DM4 is a drug-linker conjugate for antibody-drug conjugate (ADC) synthesis, combining the tubulin inhibitor DM1 with the SPDP linker[1].