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AZD3514 is a potent, orally activie and selective androgen receptor (AR) inhibitor with potential anticancer cancer activity. AZD3514 binds to the AR ligand binding domain and has selectivity for binding to AR over other nuclear hormone receptors.
AZD3514 has been shown to reduce AR protein expression, PSA synthesis and cell growth in vitro in a subclone of cells serially maintained in the presence of bicalutamide (LNCaP-CR). AZD3514 (0-30 μM/L; 24 h) reduces AR protein expression in LNCaPs and LAPC4s.
In vivo, oral dosing of AZD3514 (100mg/kg once-daily for 7 days) significantly inhibited testosterone-induced growth of sexual accessory organs in the Hershberger castrated rat assay. AZD3514 treatment also reduced AR protein in LNCaP cells maintained in steroid-depleted conditions; an effect which was evident within 6 - 8h, and maximal at 18 - 24h. Administration of AZD3514 (100 mg/kg/day orally) for 3 days to Copenhagen rats bearing R3327H Dunning prostate tumours, indicates that AZD3514 treatment also reduces tumour AR in vivo.
| Molecular Weight | 519.56 |
| Formula | C25H32F3N7O2 |
| CAS Number | 1240299-33-5 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Androgen Receptor Products |
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| Bicalutamide
Bicalutamide is an orally active non-steroidal androgen receptor antagonist (IC50 = 190 nM). |
| Ostarine
Ostarine (GTx-024 and MK-2866) is an investigational selective androgen receptor modulator (SARM) with Ki of 3.8 nM. |
| Andarine
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| Apalutamide (ARN-509)
Apalutamide (ARN-509) is a novel androgen receptor (AR) antagonist for the treatment of castration-resistant prostate cancer (CRPC). |
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