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Bicalutamide

Cat. No. M1960
Bicalutamide Structure
Synonym:

Casodex, Cosudex

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
50mg USD 35  USD35 In stock
100mg USD 50  USD50 In stock
200mg USD 70  USD70 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
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
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] Levine D, et al. Cancer. A phase II evaluation of goserelin and bicalutamide in patients with ovarian cancer in second or higher complete clinical disease remission.

[2] Furr BJ, et al. Urology. The preclinical development of bicalutamide: pharmacodynamics and mechanism of action.

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  Catalog
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Keywords: Bicalutamide, Casodex, Cosudex supplier, Androgen Receptor, inhibitors, activators


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