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AZ'6421

Names

[ CAS No. ]:
2361115-35-5

[ Name ]:
AZ'6421

Biological Activity

[Description]:

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[1].

[Related Catalog]:

Signaling Pathways >> Others >> Estrogen Receptor/ERR
Research Areas >> Cancer
Signaling Pathways >> PROTAC >> PROTAC

[Target]

IC50: 0.6 nM (ER binding); 0.4 nM (ER degradation)[1]


[In Vitro]

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.

Chemical & Physical Properties

[ Molecular Formula ]:
C52H65F3N6O7S

[ Molecular Weight ]:
975.17


Related Compounds

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