Network Version
Product Name: | Apalutamide | |
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CAS No.: | 956104-40-8 | |
Cat. No.: | HY-16060 | |
MWt: | 477.43 | |
Formula: | C21H15F4N5O2S | |
Purity : | >98% | |
Solubility: | DMSO : 50 mg/mL (104.73 mM; Need ultrasonic) | |
Mechanisms: | Target: Cancer | |
Biological Activity: | ||
Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[1]. IC50 & Target: IC50: 16 nM (Androgen receptor)[1] In Vitro: Apalutamide (ARN-509) also exhibits low micromolar affinity (IC50 3 μM) for the GABAA receptor in radioligand binding-assays and thus may potentially antagonize GABAA at therapeutic dose levels[1]. Apalutamide is a potent androgen receptor (AR) antagonist that targets the AR ligand-binding domain and prevents AR nuclear translocation, DNA binding, and transcription of AR gene targets[2]. In Vivo: Apalutamide (ARN-509) exhibits low systemic clearance, high oral bioavailability and long plasma half-life in both mouse and dog, supporting once-daily oral dosing. Consistent with its long terminal-half-life, Apalutamide steady-state plasma-levels increases in repeat-dose studies, resulting in high C24hr levels and low peak:trough ratios (ratio:2.5). Castrate male mice bearing LNCaP/AR xenograft tumors are treated with either Apalutamide at doses of 1, 10 or 30 mg/kg/day. Thirteen of 20 Apalutamide (30 mg/kg/day)-treated animals exhibit >50% reduction in tumor-volume at day 28 versus 3 of 19 MDV3100 (30 mg/kg/day)-treated mice[1]. |
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