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Bicalutamide

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Catalog No. T0380Cas No. 90357-06-5
Alias ICI-176334

Bicalutamide (ICI-176334), a synthetic, nonsteroidal antiandrogen, competitively binds to cytosolic androgen receptors in target tissues, thereby inhibiting the receptor binding of androgens.

Bicalutamide

Bicalutamide

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Purity: 99.87%
Catalog No. T0380Alias ICI-176334Cas No. 90357-06-5
Bicalutamide (ICI-176334), a synthetic, nonsteroidal antiandrogen, competitively binds to cytosolic androgen receptors in target tissues, thereby inhibiting the receptor binding of androgens.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
50 mg$32In StockIn Stock
100 mg$45In StockIn Stock
500 mg$68In StockIn Stock
1 g$85In StockIn Stock
5 g$197-In Stock
1 mL x 10 mM (in DMSO)$48In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.87%
Color:White
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Product Introduction

Bioactivity
Description
Bicalutamide (ICI-176334), a synthetic, nonsteroidal antiandrogen, competitively binds to cytosolic androgen receptors in target tissues, thereby inhibiting the receptor binding of androgens.
Targets&IC50
Androgen receptor:0.16 μM
In vivo
Single bicalutamide reduces tumor growth by 79%, at defined submaximal doses. The ridaforolimus-bicalutamide combination exhibits improved and potent antitumor activity, almost completely abrogating tumor growth. The combination is also well tolerated, as evidenced by no significant changes in body weight over the course of treatment. Plasma PSA levels are again tightly linked to tumor growth in the combination-treated mice. [3]
Kinase Assay
Whole-cell competitive binding assays: Whole-cell competitive binding assays are performed in LNCaP/AR(codon-switch) (LNCaP/AR(cs)) (harbors a mixture of exogenous wild-type AR and endogenous mutant AR (T877A)) and cells propagated in Iscove's or RPMI media supplemented with 10% fetal bovine serum, or during the assay with 10% charcoal-stripped, dextran-treated fetal bovine serum (CSS). Cells are pre-incubated with 18F-FDHT, increasing concentrations (1pM to 1 μM) of cold Bicalutamide are added, and the assay is performed to measure specific uptake of 18F-FDHT (4). IC50 values are determined using a one site binding model with least squares curve fitting and R2 > 0.99.
Cell Research
Exponentially growing C4-2 cells are plated into two 96-well plates and incubated overnight at 37 ?C. Twenty-four hours later 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). Following 72 hours culture at 37 ?C, the plates are assessed simultaneously for cell growth using the Cy qUANT Cell Proliferation Assay kit. 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.(Only for Reference)
SynonymsICI-176334
Chemical Properties
Molecular Weight430.37
FormulaC18H14F4N2O4S
Cas No.90357-06-5
SmilesCC(O)(CS(=O)(=O)C1=CC=C(F)C=C1)C(=O)NC1=CC(=C(C=C1)C#N)C(F)(F)F
Relative Density.1.52 g/cm3 (Predicted)
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 250 mg/mL (580.9 mM), Sonication is recommended.
Ethanol: 4.31 mg/mL (10.01 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.65 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.3236 mL11.6179 mL23.2358 mL116.1791 mL
5 mM0.4647 mL2.3236 mL4.6472 mL23.2358 mL
10 mM0.2324 mL1.1618 mL2.3236 mL11.6179 mL
DMSO
1mg5mg10mg50mg
20 mM0.1162 mL0.5809 mL1.1618 mL5.8090 mL
50 mM0.0465 mL0.2324 mL0.4647 mL2.3236 mL
100 mM0.0232 mL0.1162 mL0.2324 mL1.1618 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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