3042848-25-6
Chemical Structure
Mocertatug rezetecan (DAR6)
Synonym(s): HS-20089 (DAR6); GSK5733584 (DAR6)
- CAS No.: 3042848-25-6
- Formula:N/A
- Molecular Weight:N/A
SMILES: [Mocertatug rezetecan (DAR6)]
Biological Activity: Mocertatug rezetecan (DAR6) (HS-20089 (DAR6); GSK5733584 (DAR6)) is an antibody-drug conjugate (ADC) targeting B7-H4, composed of Mocertatug (HY-P991703) and MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan (HY-148668). Mocertatug rezetecan (DAR6) delivers a TOPO1 inhibitor payload. It binds to B7-H4-expressing tumor cells, triggers ADC internalization, and induces S-phase cell cycle arrest, cytotoxicity, and bystander killing effect. Mocertatug rezetecan (DAR6) exhibits dose-dependent tumor growth inhibition in breast cancer and endometrial cancer CDX models. It can be used in research related to platinum-resistant ovarian cancer, breast cancer, endometrial cancer, cholangiocarcinoma, and cervical cancer[1][2][3].
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Mocertatug rezetecan (DAR6) | Mocertatug rezetecan (DAR6) (HS-20089 (DAR6); GSK5733584 (DAR6)) is an antibody-drug conjugate (ADC) targeting B7-H4, composed of Mocertatug (HY-P991703) and MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan (HY-148668). Mocertatug rezetecan (DAR6) delivers a TOPO1 inhibitor payload. It binds to B7-H4-expressing tumor cells, triggers ADC internalization, and induces S-phase cell cycle arrest, cytotoxicity, and bystander killing effect. Mocertatug rezetecan (DAR6) exhibits dose-dependent tumor growth inhibition in breast cancer and endometrial cancer CDX models. It can be used in research related to platinum-resistant ovarian cancer, breast cancer, endometrial cancer, cholangiocarcinoma, and cervical cancer. | |||||||||||||||||||||
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Mocertatug rezetecan (DAR4) | Mocertatug rezetecan (DAR4) (HS-20089 (DAR4); GSK5733584 (DAR4)) is an antibody-drug conjugate (ADC) targeting B7-H4, composed of Mocertatug (HY-P991703) and MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan (HY-148668). Mocertatug rezetecan (DAR4) delivers a TOPO1 inhibitor payload. It binds to B7-H4-expressing tumor cells, triggers ADC internalization, and induces S-phase cell cycle arrest, cytotoxicity, and bystander killing effect. Mocertatug rezetecan (DAR4) exhibits dose-dependent tumor growth inhibition in breast cancer and endometrial cancer CDX models. It can be used in research related to platinum-resistant ovarian cancer, breast cancer, endometrial cancer, cholangiocarcinoma, and cervical cancer. | |||||||||||||||||||||
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- [1]. Zhou L, et al. The role of B7-H4 in ovarian cancer immunotherapy: current status, challenges, and perspectives. Frontiers in immunology. 2024;15:1426050. [Content Brief]
- [2]. Wu J, et al. 381O First-in-human/phase I trial of HS-20089, a B7-H4 ADC, in patients with advanced solid tumors[J]. Annals of Oncology, 2023, 34: S336.
- [3]. Waight J, et al. Non-clinical characterization of Mocertatug Rezetecan (GSK5733584), a novel B7-H4-directed antibody-drug conjugate[J]. Cancer Research, 2026, 86(7_Supplement): 4575-4575.
