topoisomerase i

Dxd (OQM5SD32BQ) is a potent inhibitor of DNA topoisomerase I with an IC50 of 0.31 μM. It is used as a conjugated drug of HER2-targeting ADC.

CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC).. CL2A-SN-38 is composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a noncleavable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. .

PNU-159682, a metabolite of anthracycline neomycin, is a DNA topoisomerase II inhibitor with excellent cytotoxicity.

MAC glucuronide phenol-linked SN-38, a pH-sensitive lactone and DNA topoisomerase I inhibitor drug linker, exhibits cytotoxicity in L540cy and Ramos cells, with IC50 values of 113 ng mL and 67 ng mL, respectively[1].

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).

MAC glucuronide α-hydroxy lactone-linked SN-38 (Topoisomerase I inhibitor) is a cytotoxic drug linker that maintains a stabilized lactone form, demonstrating efficacy against L540cy and Ramos cells with IC50 values of 99 and 105 ng mL, respectively[1].

Deruxtecan-Eribulin is a Drug-Linker Conjugate for ADC comprised of a linker and two cytotoxic molecules: Exatecan (a DNA topoisomerase I inhibitor) and Eribulin (a microtubule inhibitor). This compound is utilized in the synthesis of ADCs.

MC-GGFG-DX8951 (MC-GGFG-Exatecan) is an antibody-coupled drug (ADC) drug-linker conjugate (DLC) consisting of DX8951, a potent DNA topoisomerase I inhibitor, the linker MC, and the cleavable peptide chain GGFG, and has antitumor potential.