agents

N-(2-Hydroxypropyl)methacrylamide is utilized in the synthesis of copolymers for the targeted delivery of antileishmanial agents in [Visceral leishmaniasis].

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.

Ketoprofen (RP-19583) is a propionic acid derivative and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. It inhibits cyclo-oxygenase I and II, decreasing the formation of prostaglandin and thromboxane precursors. This reduction in prostaglandin synthesis, mediated by prostaglandin synthase, is responsible for its therapeutic effects. Additionally, Ketoprofen decreases thromboxane A2 formation via thromboxane synthase, inhibiting platelet aggregation.

Idoxuridine (Dendrid) is an analog of DEOXYURIDINE that inhibits viral DNA synthesis. The drug is used as an antiviral agent.

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.