Bavdegalutamide

Bavdegalutamide (CAS No.: 2222112-77-6) is a heterobifunctional proteolysis targeting chimera (PROTAC) compound classified as a selective androgen receptor (AR) degrader, used in targeted protein degradation research, AR signaling biology, and related prostate-derived model studies. Its mechanism of action is based on a dual-ligand scaffold that simultaneously binds AR and the cereblon (CRBN) E3 ubiquitin ligase complex via a linker, inducing receptor ubiquitination and degradation through the proteasomal pathway, thereby downregulating AR-dependent transcriptional programs and altering downstream pathway phenotypes. In cellular systems (such as VCaP prostate-derived cells), it can exhibit time- and concentration-dependent decreases in AR protein levels accompanied by reduced proliferation, while retaining degradation activity against AR mutants commonly encountered in experiments and under high-androgen backgrounds; reported cellular degradation potency is in the subnanomolar to low-nanomolar range. Typical research applications include elucidating cellular dependence on the AR pathway and mechanisms of tolerance to antagonists, validating AR as a degradable target, and comparing the pharmacological differences between “degraders—inhibitors” in drug screening workflows, with use scenarios covering cell culture and xenograft animal models; the specific concentrations or doses used in experiments typically depend on the respective experimental design and research objectives. This product is for in vitro and in vivo preclinical research use only and is not intended for any human use, clinical administration, or other non-research purposes.