ERD-308 - CAS 2320561-35-9

ERD-308 is a highly potent PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment. ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines (DC50 (concentration causing 50% of protein degradation) of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells, respectively).

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Molecular Formula
Molecular Weight


    • Specification
      • Solubility
        10 mM in DMSO
        Please store the product under the recommended conditions in the Certificate of Analysis.
        Room temperature in continental US; may vary elsewhere
        ERD-308; ERD 308; ERD308; (2S,4R)-1-[(2S)-2-[[2-[5-[ethyl-[2-[4-[6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophene-3-carbonyl]phenoxy]ethyl]amino]pentoxy]acetyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide
    • Properties
      • InChI Key
        Canonical SMILES
    • Reference Reading
      • 1. Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER)
        Jiantao Hu, Biao Hu, Mingliang Wang, Fuming Xu, Bukeyan Miao, Chao-Yie Yang, Mi Wang, Zhaomin Liu, Daniel F Hayes, Krishnapriya Chinnaswamy, James Delproposto, Jeanne Stuckey, Shaomeng Wang J Med Chem. 2019 Feb 14;62(3):1420-1442. doi: 10.1021/acs.jmedchem.8b01572.Epub 2019 Jan 18.
        The estrogen receptor (ER) is a validated target for the treatment of estrogen receptor-positive (ER+) breast cancer. Here, we describe the design, synthesis, and extensive structure-activity relationship (SAR) studies of small-molecule ERα degraders based on the proteolysis targeting chimeras (PROTAC) concept. Our efforts have resulted in the discovery of highly potent and effective PROTAC ER degraders, as exemplified by ERD-308 (32). ERD-308 achieves DC50 (concentration causing 50% of protein degradation) values of 0.17 and 0.43 nM in MCF-7 and T47D ER+ breast cancer cell lines, respectively, and induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines. Significantly, 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. Further optimization of ERD-308 may lead to a new therapy for advanced ER+ breast cancer.
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Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
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