AZD0516 

AZD0516 is a first-in-class antibody-drug conjugate (ADC) targeting six-transmembrane epithelial antigen of the prostate-2 (STEAP2). The anti-STEAP2 monoclonal antibody (mAb) is conjugated via interchain cysteines to a maleimide-reactive, β-glucuronidase-cleavable linker (HY-173635) bearing the topoisomerase 1 inhibitor, Exatecan (HY-13631). AZD0516 can be used for the study of prostate cancer^[1].

In vitro cytotoxicity assays with AZD0516 revealed IC₅₀ values in the low nM range and the ADC induced both single- and double-strand DNA breaks, characteristic of the proposed primary mechanism of action (MoA) of the TOP1i payload, namely, DNA damage and apoptotic cell death^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

The mechanistic and pharmacodynamic effects of AZD0516 are observed in a prostate cancer cell line-derived xenograft (CDX) model via a dose-dependent increase in positive staining for γH2AX foci, indicative of DNA damage. AZD0516 monotherapy administration in prostate cancer CDX and patient-derived xenograft models led to sustained tumor responses^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

162163 (average)

Liquid

Colorless to light yellow

[AZD0516]

Shipping with dry ice.

-80°C, protect from light

• [1]. 1158-Preclinical characterization of AZD0516, a novel STEAP2 antibody-drug conjugate (ADC) for the treatment of prostate cancer. AACR Annual Meeting 2025 Itinerary Planner Home.

  [2]. Darlene Monlish, et al. Abstract 1158: Preclinical characterization of AZD0516, a novel STEAP2 antibody-drug conjugate (ADC) for the treatment of prostate cancer. Cancer Res (2025) 85 (8_Supplement_1): 1158.