tumor xenograft model

AU-15330 is a protein hydrolysis-targeted chimeric (PROTAC) degrader of the SWI SNF ATPase subunits SMARCA2 and SMARCA4.AU-15330 potently inhibits tumor growth in a prostate cancer xenograft model and acts synergistically with the AR antagonist enzalutamide.AU-15330 shows partial therapeutic efficacy and non-toxicity with the AR antagonist enzalutamide in a desmoplasia-resistant prostate cancer (CRPC) model. AU-15330 showed partial therapeutic efficacy in a denervation-resistant prostate cancer (CRPC) model and AU-15330 was characterized by non-toxicity.

ARD-61 is a potent and specific PROTAC androgen receptor (AR) degrader, exhibiting high effectiveness. It effectively induces the degradation of AR and progesterone receptors (PR) in AR+ cancer cell lines, leading to apoptosis. Additionally, ARD-61 demonstrates significant tumor growth inhibition in the MDA-MB-453 xenograft model in mice.

YN14 is a highly potent and selective KRASG12C proteolysis targeting chimera (PROTAC) capable of forming a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). It exhibits antiproliferative effects, significantly inhibiting the growth of KRASG12C-mutant cancer cells, and demonstrates tumor regression with tumor growth inhibition (TGI%) rates exceeding 100% in the MIA PaCa-2 xenograft model.

ERD-3111 (Compound 44), an orally active PROTAC ERα degrader (DC50: 0.5 nM), exhibits efficacy in inhibiting tumor growth in both the parental MCF-7 xenograft model harboring wild-type ER and two ESR1-mutated mouse models. This compound has utility in the investigation of ER+ breast cancer [1].