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Bicalutamide (marketed as Casodex, Cosudex, Calutide, Kalumid) 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 |
|---|
| LGD-3303
LGD-3303 is a nonsteroidal, nonaromatizable selective androgen receptor ligand that binds to the androgen receptor with high affinity in a radiolabeled to competitive binding assay (Ki=0.9 nM). |
| Ar-V7-IN-1
Ar-V7-IN-1 is a potent inhibitor of Ar-V7. AR-V7 is a hormone-independent splice variant of the androgen receptor. Ar-V7-IN-1 has the potential for the research of various indications such as prostate cancer. |
| SC912
SC912 is a potent and selective AR-V7 inhibitor with IC50 of 0.36 μM. SC912 binds directly to AR-FL and AR-V7 proteins, inhibites nuclear localization and chromatin binding capabilities. SC912 exerts anticancer activity through inhibition of proliferation, induction of cell cycle arrest and apoptosis. |
| A4B17
A4B17 is an androgen receptor N-terminal inhibitor, which can be used for the research of androgen-responsive prostate cancer. |
| AZ'3137
AZ‘3137 is an orally active PROTAC-type androgen receptor (AR) degrader, with a DC50 value of 22 nM. |
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