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CAS: 2521299-80-7
Chemical Name: (2S,4R)-1-((2S)-2-(6-(4-(((1R,4R)-5,6-Bis(4-hydroxyphenyl)-N-(2,2,2-trifluoroethyl)-7-oxabicyclo[2.2.1]hept-5-ene)-2-sulfonamido)phenoxy)hexanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide
Purity: >98% (HPLC)
Novel selective ERα degrader (Ki values: ERα 5.08 µM and Erβ 26.20 µM), degrading both the WT and mutant Erα in ER+ BC cell lines (MCF-7), inhibiting nascent RNA synthesis of several ERα target genes, such as IGFBP4 and GREB1
Reference:
https://pubs.acs.org/doi/10.1021/acs.jmedchem.2c02032
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