Shelf life (days): 1460
Info: A PROTAC that drives BRM and BRG1 degradation; induces degradation of BRM and BRG1 in HeLa cervical cancer cells at 1 µM but also induces degradation of PBRM1 at the same concentration; decreases proliferation in a panel of 14 cancer cell lines (IC50s = 0.392-28.85 nM); reduces protein levels of FOXA1, ERG, Myc, and prostate-specific antigen in VCaP cells at 1 µM for 24 hours; reduces tumor volume in a VCaP mouse xenograft model
Formulation: A solid
Formal Name: (2S,4R)-1-((S)-2-(2-(4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide
Purity: ≥98%
Formula Markup: C39H49N9O5S
Formula Weight: 755.939
CAS Number: 2380274-50-8