PROTAC ERα Degrader-4

Names

[ CAS No. ]:
2521299-80-7

[ Name ]:
PROTAC ERα Degrader-4

Biological Activity

[Description]:

PROTAC ERα Degrader-4 is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER+ breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.

[Related Catalog]:

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

[Target]

ERα:5.08 μM (Ki)

ERβ:26.20 μM (Ki)


[References]

[1]. Xie B, et.al. Discovery of a Novel Class of PROTACs as Potent and Selective Estrogen Receptor α Degraders to Overcome Endocrine-Resistant Breast Cancer In Vitro and In Vivo. J Med Chem. 2023 May 25;66(10):6631-6651.  

Chemical & Physical Properties

[ Molecular Formula ]:
C55H62F3N5O10S2

[ Molecular Weight ]:
1074.23

Related Compounds

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