traditional cytotoxic agents

Taltobulin trifluoroacetate is a synthetic analogue of the tripeptide hemiasterlin, is a potent agent of antimicrotubule that circumvents P-glycoprotein-mediated resistance in vitro and in vivo.

C-11 is a tubulin inhibitor and functions as an ADC cytotoxin, exhibiting cytotoxicity for carcinoma cell lines.

Isofistularin-3, a direct DNA-competitive DNMT1 inhibitor with an IC50 of 13.5 μM, functions as a DNA demethylating agent, leading to cell cycle arrest and increased sensitivity to TRAIL in cancer cells. Additionally, it can be employed as an ADC cytotoxin.

Mensacarcin, a highly complex polyketide compound, exhibits multifaceted effects on cellular processes. Specifically, it targets mitochondria, perturbs energy metabolism within these organelles, and activates caspase-dependent apoptotic pathways. Functionally, Mensacarcin can serve as a cytotoxic constituent in antibody-drug conjugates (ADCs). Furthermore, this antibiotic compound displays broad-spectrum inhibition of cell growth across various cancer cell lines and demonstrates potent induction of apoptosis in melanoma cells.

β-Amanitin, a cyclic peptide toxin found in the poisonous Amanita phalloides mushroom, inhibits eukaryotic RNA polymerase II and III, thereby disrupting protein synthesis.

alpha-Amanitin (alpha-Amanitin) is the lethal toxin in Trichoderma viride and acts in vivo via the enterohepatic circulation and transport system. alpha-Amanitin induces cell death and can be used in the synthesis of ADCs. alpha-Amanitin has been shown to induce cell death and can be used in the synthesis of ADCs.

Rebeccamycin is an antitumor antibiotic+ inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I. It also has a negligible effect on protein kinase C and topoisomerase II.

AmPEG6C2-Aur0131 is a drug-linker conjugate designed for anti-CXCR4 ADC applications, showcasing potent antitumor activity. It incorporates Aur0131, an auristatin-based microtubule inhibitor, connected through the non-cleavable AmPEG6C2 linker.

Cyclooctyne-O-PFP ester is utilized as an ADC cytotoxin to link antibodies and linkers [1].

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].

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.

MC-Val-Cit-PAB-clindamycin is an antibody-drug conjugate (ADC) linker combining the potent antitumor properties of clindamycin, a protein synthesis inhibitor, with the ADC linker MC-Val-Cit-PAB, thereby enhancing its cancer cell targeting and killing effectiveness.

MC-Val-Cit-PAB-dimethylDNA31 is a drug-linker conjugate employed in antibody-drug conjugates (ADCs) that exhibits robust antitumor efficacy. This conjugate utilizes the ADC linker, MC-Val-Cit-PAB, to connect with the potent antitumor agent dimethylDNA31, which also demonstrates significant bactericidal activity against both persister and stationary-phase [Staphylococcus aureus].

MC-Val-Cit-PAB-Retapamulin is a drug-linker conjugate used in antibody-drug conjugates (ADC) that exhibits potent antitumor activity. It employs Retapamulin, a ribosome inhibitor, connected via the ADC linker MC-Val-Cit-PAB.

MC-Val-Cit-PAB-rifabutin is a drug-linker conjugate for antibody-drug conjugates (ADC), featuring the potent antitumor agent rifabutin (a DNA-dependent RNA polymerase inhibitor) connected via the MC-Val-Cit-PAB ADC linker, which endows it with significant antitumor activity.

MC-Val-Cit-PAB-tubulysin5a is a drug-linker conjugate for ADC with potent antitumor activity by using tubulysin5a (a tubulin inhibitor), linked via the ADC linker MC-Val-Cit-PAB.

MC-Val-Cit-PAB-vinblastine is a potent antitumor drug-linker conjugate for Antibody-Drug Conjugates (ADC), featuring vinblastine (a microtubule protein inhibitor) connected through the MC-Val-Cit-PAB [ADC linker].

MC-VC-PABC-DNA31 is a drug-linker conjugate designed for Antibody-Drug Conjugates (ADC), exhibiting potent antitumor activity. It utilizes DNA31, a powerful inhibitor of RNA polymerase, connected via the MC-VC-PABC ADC linker.

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.

AcLysValCit-PABC-DMAE-SW-163D is a drug-linker conjugate for antibody-drug conjugates (ADCs), incorporating the natural bis-intercalator SW-163D through an AcLysValCit-PABC-DMAE linker[1].

VCP-Eribulin, an Eribulin-based drug for antibody conjugates[1], combines the VCP (ADCs linker) with Eribulin, a distinct microtubule inhibitor used in cancer treatments[2].

Azonafide-PEABA is a drug moiety with cytotoxic [1].