ZN-c5 hydrochloride is a selective and orally active estrogen receptor degrader. ZN-c5 hydrochloride exhibits high potency in the cellular assay (MCF-7, IC50 = 0.3 nM) and binds with high affinity to ERα and ERβ ( IC50 = 0.4 nM and 0.8 nM, respectively). ZN-c5 hydrochloride inhibits tumor growth in MCF-7 mouse xenograft model and WHIM20 xenograft model. ZN-c5 hydrochloride can be used for the study of breast cancer [1].
In Vivo, ZN-c5 (1-40 mg/kg, p.o., once daily, 28 days) hydrochloride shows significant tumor growth inhibition in MCF-7 mouse xenograft model[1]. ZN-c5 (40 mg/kg, p.o., once daily, 90 days) hydrochloride induces tumor growth inhibition in the WHIM20 xenograft model (an ESR1 mutant model (Y537S))[1].
In Vitro, ZN-c5 (100 nM, 24 h) hydrochloride induces ERα degradation in breast cancer cell lines (MCF-7, ZR-75-1, CAMA-1, HCC1500 and HCC1428 cells)[1].
References:
[1]. Hegde SG, et al. Discovery of ZN-c5, an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) with Improved Pharmacokinetics. J Med Chem. 2025 Jul 24;68(14):14740-14755.
In Vivo, ZN-c5 (1-40 mg/kg, p.o., once daily, 28 days) hydrochloride shows significant tumor growth inhibition in MCF-7 mouse xenograft model[1]. ZN-c5 (40 mg/kg, p.o., once daily, 90 days) hydrochloride induces tumor growth inhibition in the WHIM20 xenograft model (an ESR1 mutant model (Y537S))[1].
In Vitro, ZN-c5 (100 nM, 24 h) hydrochloride induces ERα degradation in breast cancer cell lines (MCF-7, ZR-75-1, CAMA-1, HCC1500 and HCC1428 cells)[1].
References:
[1]. Hegde SG, et al. Discovery of ZN-c5, an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) with Improved Pharmacokinetics. J Med Chem. 2025 Jul 24;68(14):14740-14755.