AZ'6421 acts as Protcolysis Targeting Chimera (PROTAC) to selectively degrade estrogen receptor alpha. AZ'6421 has a potent anti-tumour effect to inhibit the uncontrolled cellular proliferation which arises from malignant disease. AZ'6421 can be used for the research of cancer such as breast cancer.
AZ'6421 (example 72) exhibits anti-tumour activity via the ability to degrade the estrogen receptor in a number of different breast cancer cell-lines (MCF-7, CAMA-I, and BT474)[1].AZ'6421 (0.3 μM) has ER binding and ER degradation with IC50 values of 0.6 nM and 0.4 nM, respectively in MCF-7 cell lines[1].
References:
[1]. Bin Yang, et al. Compounds and their use in treating cancer. Patent WO2019123367A1.