(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.
|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.|
|Incubation time||72 hours|
|Animal models||Male nude mice bearing C4-2 cells|
|Formulation||4% ethanol, 5% Tween 80, and 5% propylene glycol|
|Administration||Administered via p.o.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
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