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.

Vipivotide tetraxetan (PSMA-617) is a highly potent inhibitor of prostate-specific membrane antigen (PSMA) with a Ki of 0.37 nM.

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

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.

Mc-VC-PAB-SN38 consists of a cleavable ADC linker (Mc-VC-PAB) and SN38, which is part of an antibody-coupled reactive molecule commonly used to synthesize antibody-coupled reactive molecules (ADCs) that target sites of action.

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.

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].

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.

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.

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.

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.

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

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-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.

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).

MP-PEG4-Val-Lys-Gly-7-MAD-MDCPT is a Camptothecin-linker and a drug-linker conjugate for antibody-drug conjugate (ADC).

MC-VC-PAB-MMAD is a conjugate for antibody-drug conjugates (ADCs) that exhibits potent antitumor activity by employing MMAD, a powerful tubulin inhibitor, connected through the cleavable ADC linker MC-VC-PAB [1].

Glucocorticoid receptor agonist-1 Ala-Ala-Mal (compound 88), a glucocorticosteroid and glucocorticoid receptor agonist, can be conjugated with Adalimumab to formulate an ADC [1].

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

TLR7 8 agonist 4 hydroxy-PEG10-acid [compound 9] is a drug-linker conjugate used in antibody-drug conjugates (ADC), exhibiting remarkable antitumor activity. It utilizes TLR7 8 agonist 4, a potent activator of TLR7 8, linked to hydroxy-PEG10-acid via a cleavable bond, demonstrating promising pharmaceutical potential in ADC-based therapeutics.

Azido-PEG4-Val-Cit-PAB-MMAE is a drug-linker conjugate for antibody-drug conjugates (ADCs), incorporating the tubulin inhibitor monomethyl auristatin E (MMAE) and linked via the cleavable Azido-PEG4-Val-Cit-PAB-OH.

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.

SC-VC-PAB-MMAE is a potent antitumor drug-linker conjugate for antibody-drug conjugates (ADCs), consisting of the anti-mitotic agent monomethyl auristatin E (MMAE, a tubulin inhibitor) linked via the cleavable linker SC-VC-PAB[1].

MC-VC-PABC-Aur0101 is a potent anticancer drug-linker conjugate for Antibody-Drug Conjugates (ADCs), incorporating Aur0101, an auristatin microtubule inhibitor, linked via the MC-VC-PABC linker to boost antitumor efficacy.

Daunorubicinol, a potent antitumor drug-linker conjugate for antibody-drug conjugate (ADC) applications, utilizes Aur0101 (DNA Topoisomerase II inhibitor) connected through the ADC linker[1].

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

SPB is a potent anti-inflammatory drug-linker conjugate for Antibody-Drug Conjugates (ADC), utilizing Xanthotoxol connected through the ADC linker.

Mc-Val-Cit-PAB-Gefitinib chloride is a conjugate agent-linker for antibody-drug conjugates (ADCs) that combines Gefitinib, an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, with the proprietary ADC linker Mc-Val-Cit-PAB [1].

Mal-PEG8-Val-Cit-PAB-MMAF, a drug-linker conjugate utilized for antibody-drug conjugates (ADCs), includes a cleavable linker system and the potent tubulin inhibitor monomethyl auristatin F (MMAF), designed for targeted cancer therapy.

CL2E-SN-38 TFA, a structurally stable and highly releasable antibody drug conjugate (ADC), comprises SN-38, the active metabolite of Irinotecan derived from camptothecins, known for its Topoisomerase I inhibitory activity [1].

Azide-PEG4-VC-PAB-Doxorubicin is an agent-linker conjugate used in antibody-drug conjugate (ADC) applications, comprising the cytotoxic anthracycline antibiotic Doxorubicin linked through the Azide-PEG4-VC-PAB linker [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].

β-Glucuronide-dPBD-PEG5-NH2 TFA is a β-glucuronide-linked pyrrolobenzodiazepine dimer used in the synthesis of the antibody-drug conjugate (ADC) cIRCR201-dPBD, employing a cleavable β-glucuronide linkage. It serves as a proagent to reduce side effects, induce apoptosis, and arrest the cell cycle, exhibiting antitumor activity [1].

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, utilizing Modified MMAF, a tubulin inhibitor, connected via a noncleavable MC-Alkyl-Hydrazine linkage[1].

OH-Glu-Val-Cit-PAB-MMAE is a compound consisting of a cleavable ADC linker (OH-Glu-Val-Cit-PAB) and a potent tubulin inhibitor (MMAE), used in the synthesis of antibody-drug conjugates (ADCs) [1].

Val-Ala-PAB-MMAE is a drug-linker conjugate used in antibody-drug conjugates (ADCs), consisting of the ADC linker Val-Ala-PAB and the cytotoxic agent monomethyl auristatin E (MMAE), which acts as a potent tubulin inhibitor.

Mal-PEG8-amide-Val-Ala-(4-NH2)-Exatecan is a conjugated compound used in the synthesis of antibody-drug conjugates (ADCs), featuring a topoisomerase inhibitor derivative linked via a linker to a specific ligand unit[1].

MC-Val-Cit-PAB-Auristatin E is an antibody-drug conjugate (ADC) linker compound with Auristatin E, a potent cytotoxic tubulin modifier, attached via the MC-Val-Cit-PAB linker, demonstrating significant antitumor activity.

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].

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

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

DBCO-PEG4-GGFG-Dxd is a conjugate used in antibody-drug conjugates (ADCs) exhibiting potent antitumor activity. It incorporates Dxd, a DNA topoisomerase I inhibitor, connected through the cleavable linker DBCO-PEG4-GGFG [1]. This compound functions as a click chemistry reagent, featuring a DBCO group capable of strain-promoted alkyne-azide cycloaddition (SPAAC) with azide-containing molecules.

mDPR-Val-Cit-PAB-MMAE TFA is a drug-linker conjugate for antibody-drug conjugates (ADC), comprising the tubulin polymerization inhibitor MMAE coupled with an ADC-specific peptide linker (Val-Cit-PAB) [1].

Val-Ala-PABC-Exatecan trifluoroacetate is a drug-linker conjugate for antibody-drug conjugates (ADC), comprising a cleavable Tesirine linker, Val-Ala-PABC, and the topoisomerase I inhibitor Exatecan. This compound facilitates the synthesis of ADC molecules, including Mal-PEGn-amide-va-Exatecan [1].

PDS-MMAE (Compound 5') is a modified version of MMAE, designed for the synthesis of conjugates that bind to neurotensin receptors [1].