Formulation: A solid
Formal Name: N-[trans-3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]-4-[4-[[1-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-4-piperidinyl]methyl]-1-piperazinyl]-benzamide
Purity: ≥98%
Formula Markup: C45H50ClN7O6
Formula Weight: 820,4
Shelf life (days): 1460
CAS Number: 2222111-87-5
Notes: ARD-2128 is a proteolysis targeting chimera (PROTAC) that is composed of an androgen receptor (AR) antagonist and thalidomide, a ligand for the E3 ubiquitin ligase cereblon.{51817} It induces degradation of ARs in VCaP and LNCaP prostate cancer cells with half-maximal degradation (DC50) concentrations of 0.3 and 8.3 nM, respectively, and inhibits the proliferation of VCaP and LNCaP cells (IC50s = 4 and 5 nM, respectively). ARD-2128 (10 mg/kg) decreases intratumoral protein levels of AR and the mRNA encoding puromycin-sensitive aminopeptidase (PSA), transmembrane serine protease 2 (TMPRSS2), and FK-506 binding protein 5 (FKBP5), but not mRNA encoding AR, in a VCaP mouse xenograft model. It reduces tumor volume in the same mice when administered at doses of 20 or 40 mg/kg per day.
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