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ERD-308

Chemical Structure : ERD-308

CAS No.: 2320561-35-9

ERD-308 (ERD308)

Catalog No.: PC-73165Not For Human Use, Lab Use Only.

ERD-308 (ERD308) is a highly potent estrogen receptor (ER) PROTAC degrader with DC50 of 0.17 and 0.43 nM in MCF-7 and T47D ER+ breast cancer cell lines, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

ERD-308 (ERD308) is a highly potent estrogen receptor (ER) PROTAC degrader with DC50 of 0.17 and 0.43 nM in MCF-7 and T47D ER+ breast cancer cell lines, respectively.
ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM in MCF-7 and T47D ER+ breast cancer cell lines.
ERD-308 induces more complete ER degradation than fulvestrant, the only approved selective ER degrader (SERD), and is more effective in inhibition of cell proliferation than fulvestrant in MCF-7 cells.

Physicochemical Properties

M.Wt 1004.26
Formula C55H65N5O9S2
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

(2S,4R)-1-((S)-2-(2-((5-(Ethyl(2-(4-(6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thiophene-3-carbonyl)phenoxy)ethyl)amino)pentyl)oxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

References

1. Jiantao Hu, et al. J Med Chem. 2019 Feb 14;62(3):1420-1442.

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