ERD-1233 (ERD1233)

Chemical Structure : ERD-1233

Catalog No.: PC-24557Not For Human Use, Lab Use Only.

ERD-1233 is a potent and orally efficacious PROTAC degrader of estrogen receptor α (ERα) with DC50 of 0.9 nM in MCF-7 cell line, Dmax=100%.

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Biological Activity

ERD-1233 is a potent and orally efficacious PROTAC degrader of estrogen receptor α (ERα) with DC50 of 0.9 nM in MCF-7 cell line, Dmax=100%.
ERD-1233 potently and effectively reduces the ERα protein in vitro and achieves excellent oral bioavailability in mice and rats.
Oral administration of ERD-1233 effectively reduces ER protein in ER+ tumors and achieves tumor regression in the ER wild-type MCF-7 xenograft tumor model and strong tumor growth inhibition in the ESR1Y537S mutated model in mice.

Physicochemical Properties

M.Wt	807.99
Formula	C49H53N5O6
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(3S)-3-((5aR)-7-((8-(4-((1R,2S)-6-Hydroxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenyl)-1-oxa-8-azaspiro[4.5]decan-3-yl)methyl)-1-oxo-1,3,5,5a,6,7,8,9-octahydro-2H-pyrazino[1′,2′:4,5][1,4]oxazino[2,3-e]isoindol-2-yl)piperidine-2,6-dione

References

1. Acharyya RK, et al. J Med Chem. 2024 Nov 14;67(21):19010-19037.

ERD-1233 (ERD1233)

Biological Activity

Physicochemical Properties

References

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