Free shipping on all orders over $ 500

(R)-Bicalutamide

Cat. No. M3234
(R)-Bicalutamide Structure
Size Price Availability
25mg USD 120  USD120 Out of stock
10mg USD 150  USD150 Out of stock
50mg USD 530  USD530 Out of stock
100mg USD 850  USD850 Out of stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

(R)-Bicalutamide is an active competitive non-steroidal androgen receptor antagonist with an IC50 of 0.17 μM for MDA 453 cells. (R)-Bicalutamide possesses virtually all activities. (R)-Bicalutamide is the leading antiandrogen. (R)-Bicalutamide is used for the treatment of prostate cancer and breast cancer. (R)-Bicalutamide prevents the activation of the androgen receptor and subsequent upregulation of androgen responsive genes by androgenic hormones. In addition, (R)-bicalutamide accelerates the degradation of the androgen receptor.

Protocol (for reference only)
Cell Experiment
Cell lines C4-2 cell
Preparation method Plating exponentially growing C4-2 cells into two 96-well plates and incubating overnight at 37 ˚C. One plate is aspirated and stored at -80 ˚C and the other treated with 10-fold serial concentrations of ridaforolimus (1000 nM to 0.0001 nM) or vehicle (ethanol) after 24h. Following 72 hours culture at 37 ˚C, using the Cy qUANT Cell Proliferation Assay kit the plates to assess simultaneously for cell growth. Bicalutamide and Ridaforolimus combination proliferation assays are performed similarly except cell growth is determined as the change in cell number between vehicle control and compound treated cells after 72 hours in culture.
Concentrations 0-1 μM
Incubation time 72 hours
Animal Experiment
Animal models Male nude mice bearing C4-2 cells
Formulation 4% ethanol, 5% Tween 80, and 5% propylene glycol
Dosages 10 mg/kg
Administration Administered via p.o.
Chemical Information
Molecular Weight 430.37
Formula C18H14F4N2O4S
CAS Number 113299-40-4
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] William U Shipley, et al. Radiation with or without Antiandrogen Therapy in Recurrent Prostate Cancer

[2] Hongli Liu, et al. Molecular mechanism of R-bicalutamide switching from androgen receptor antagonist to agonist induced by amino acid mutations using molecular dynamics simulations and free energy calculation

[3] Hongli Liu, et al. Interaction mechanism exploration of R-bicalutamide/S-1 with WT/W741L AR using molecular dynamics simulations

[4] Sara Pignatta, et al. Prolonged exposure to (R)-bicalutamide generates a LNCaP subclone with alteration of mitochondrial genome

[5] Ian D Cockshott. Bicalutamide: clinical pharmacokinetics and metabolism

Related Androgen Receptor Products
Androstenone

Androstenone is a steroid pheromone and also a metabolite of androgens.

(Des-Glu5)-ACTH (1-24) (human, bovine, rat)

(Des-Glu5)-ACTH (1-24) (human, bovine, rat) is an analogue of Adrenocorticotropic hormone (ACTH).

Acetyl-ACTH (2-24) (human, bovine, rat)

Acetyl-ACTH (2-24) (human, bovine, rat) is a fragment of proopiomelanocortin (POMC) peptide.

Acetyl-ACTH (3-24) (human, bovine, rat)

Acetyl-ACTH (3-24) (human, bovine, rat) is a fragment of proopiomelanocortin (POMC) peptide.

Acetyl-ACTH (4-24) (human, bovine, rat)

Acetyl-ACTH (4-24) (human, bovine, rat) is a fragment of proopiomelanocortin (POMC) peptide.

  Catalog
Abmole Inhibitor Catalog




Keywords: (R)-Bicalutamide supplier, Androgen Receptor, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.