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Bicalutamide is a non-steriodal Androgen Receptor (AR) inhibitor. Bicalutamide (CDX) is inhibited by non-genomic, transcription-independent stimulation of PI3K/AKT phosphorylation by androgens. Bicalutamide displays peripheral selectivity and does not effect serum levels of LH and testosterone. Bicalutamide exhibits potent anticancer activity in vivo. Bicalutamide acts as a pure anti-androgen by binding to the androgen receptor (AR) and preventing the activation of the AR and subsequent upregulation of androgen responsive genes by androgenic hormones. In addition, bicalutamide accelerates the degradation of the androgen receptor. Bicalutamide is induces cell death by a pathway that is independent of changes in mitochondrial membrane potential and Bcl-2 action. Bicalutamide is currently tested for treatment of andogen receptor positive ER-/PR- metastatic breast cancer.
| Molecular Weight | 430.37 |
| Formula | C18H14F4N2O4S |
| CAS Number | 90357-06-5 |
| Solubility (25°C) | DMSO 48 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 |
|---|
| N-Desmethyl Enzalutamide
N- Desmethyl Enzalutamide |
| Norelgestromin
Norgestimate and its metabolite norelgestromin possess weak androgen-like properties. |
| MDV3100
MDV3100 is an orally bioavailable, organic, non-steroidal small molecule targeting the androgen receptor (AR) with potential antineoplastic activity. |
| Ostarine
Ostarine (GTx-024 and MK-2866) is an investigational selective androgen receptor modulator (SARM) with Ki of 3.8 nM. |
| Andarine
Andarine (GTx-007, S-4) is a selective nonsteroidal androgen receptor (AR) agonist with Ki of 4 nM. |
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