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GNE-502

Names

[ CAS No. ]:
1953134-16-1

[ Name ]:
GNE-502

Biological Activity

[Description]:

GNE-502 is an orally active and potent degrader for estrogen receptor (ER). GNE-502 can be used for the research of breast cancer[1].

[Related Catalog]:

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

[Target]

ER[1]


[In Vivo]

GNE-502 (10 and 100 mg/kg; p.o.) possesses sufficient oral exposure to be tested in a WT MCF7 tumor xenograft model[1]. ..GNE-502 shows dose dependent tumor growth inhibition at 10 mg/kg and 30 mg/kg, with tumor stasis at 100 mg/kg[1]. Animal Model: Mouse[1] Dosage: 10 and 100 mg/kg (Pharmacokinetic Analysis) Administration: P.o. Result: Possessed sufficient oral exposure to be tested in a WT MCF7 tumor xenograft model.

[References]

[1]. Zbieg JR, et al. Discovery of GNE-502 as an Orally Bioavailable and Potent Degrader for Estrogen Receptor Positive Breast Cancer [published online ahead of print, 2021 Aug 20]. Bioorg Med Chem Lett. 2021;128335.

Chemical & Physical Properties

[ Molecular Formula ]:
C25H30FN3O3S

[ Molecular Weight ]:
471.59

Related Compounds