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(R)-Bicalutamide 

Cat. No.: HY-108250 Purity: 99.93%
Handling Instructions

(R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgen receptor (AR) antagonist, with an antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer.

For research use only. We do not sell to patients.

(R)-Bicalutamide Chemical Structure

(R)-Bicalutamide Chemical Structure

CAS No. : 113299-40-4

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Description

(R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgen receptor (AR) antagonist, with an antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer[1][2].

IC50 & Target

AR[1]

In Vitro

Bicalutamide (HY-14249) is available as a racemic mixture. The R isomer (R-bicalutamide) has an ≈30-fold higher binding affinity to the AR than the S isomer[1].
(R)-bicalutamide (0.02-20 μM) reduces naïve LNCaP cells survival in a dose-dependent[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

Cell Line: LNCaP cells, LNCaP-Rbic cells
Concentration: 0.02 μM, 0.2 μM, 2 μM, 20 μM
Incubation Time: 144 hours
Result: Reduced naïve LNCaP cells survival in a dose-dependent, with an IC 50 value of about 7μM; exerted a poor antiproliferative effect on LNCaP-Rbic.
In Vivo

(R)-Bicalutamide (10 mg/kg; i.g.; daily; for 4 days) has antitumor efficacy in VCaP xenografts mice[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CD1 male nude (nu/nu) mice, with VCaP xenografts[3]
Dosage: 10 mg/kg
Administration: Orally gavage, daily, for 4 consecutive weeks
Result: Suppressed tumor growth.
Molecular Weight

430.37

Formula

C₁₈H₁₄F₄N₂O₄S

CAS No.

113299-40-4

SMILES

O=C(NC1=CC=C(C#N)C(C(F)(F)F)=C1)[[email protected]@](C)(O)CS(=O)(C2=CC=C(F)C=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (232.36 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3236 mL 11.6179 mL 23.2358 mL
5 mM 0.4647 mL 2.3236 mL 4.6472 mL
10 mM 0.2324 mL 1.1618 mL 2.3236 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.81 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.81 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.81 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

(R)-BicalutamideAndrogen ReceptorantiandrogenprostatecancerantineoplasticmodulatingandrogenreceptorLNCaP cellsInhibitorinhibitorinhibit

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(R)-Bicalutamide
Cat. No.:
HY-108250
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