AU-24118 is a potent, selective, and orally bioavailable degrader of mSWI/SNF ATPases (SMARCA2, SMARCA4) and PBRM1.
AU-24118 integrates a bait moiety binding to the bromodomains of SMARCA2 and SMARCA4, along with a ligand moiety for CRBN ligase.
AU-24118 selectively degraded SMARCA2, SMARCA4, and PBRM1 in VCaP prostate cancer cells, through the CRBN-based proteasomal degradation machinery.
AU-24118 induces tumor regression as a single agent, as well as in combination with enzalutamide, in a VCaP CRPC model.
has increased efficacy compared to AU-15330 in terms of both target degradation efficiency as well as potency in vivo.
