5N-Bicalutamide is a highly potent nonsteroidal antiandrogen (NSAA) and an analog of bicalutamide designed to overcome resistance in prostate cancer. It shows significantly improved antiandrogenic activity compared to bicalutamide, with reported IC₅₀ values for AR (androgen receptor) binding in the low nanomolar range — for example, 5N-Bicalutamide demonstrated an IC₅₀ of 3.8 nM for AR binding versus 162 nM for bicalutamide in in vitro assays. It functions as a competitive AR antagonist, inhibiting androgen-induced AR activation and downstream gene expression.
MedKoo Cat#: 563978
Name: 5N-Bicalutamide
CAS#: 1845688-96-1 (racemic)
Chemical Formula: C17H13F4N3O4S
Exact Mass: 431.0563
Molecular Weight: 431.36
Elemental Analysis: C, 47.34; H, 3.04; F, 17.62; N, 9.74; O, 14.84; S, 7.43
Preclinical studies indicate it retains activity against certain bicalutamide-resistant AR mutants, suggesting promise for castration-resistant prostate cancer (CRPC) treatment. However, detailed pharmacokinetic and in vivo efficacy data remain limited to early-stage animal models, highlighting the need for further clinical investigation.
The following data is based on the product molecular weight 431.36 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
