Referencia número: HY-108250

(R)-Bicalutamide

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

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Pureza: 99.95%
No. CAS: 113299-40-4
Fòrmula: C₁₈H₁₄F₄N₂O₄S
Peso molecular:430.37

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

(R)-Bicalutamide Chemical Structure

No. CAS: 113299-40-4

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

AR^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	>25 μM Compound: R-(1)	Inhibition of human ERG expressed in CHO cells by whole-cell voltage-clamp analysis Inhibition of human ERG expressed in CHO cells by whole-cell voltage-clamp analysis	[PMID: 31288149]
CWR22R	IC₅₀	37.4 μM Compound: (R)-12a, (R)-Bic	Inhibition of cell survival in human CWR22Rv1 cells after 144 hrs by TUNEL assay Inhibition of cell survival in human CWR22Rv1 cells after 144 hrs by TUNEL assay	[PMID: 25121586]
CWR22R	IC₅₀	44.588 μM Compound: 45a; R-Bicalutamide	Antiproliferative activity against human 22Rv1 cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay Antiproliferative activity against human 22Rv1 cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	[PMID: 27131065]
CWR22R	IC₅₀	46.25 μM Compound: 45a; R-Bicalutamide	Antiproliferative activity against human 22Rv1 cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay Antiproliferative activity against human 22Rv1 cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	[PMID: 27131065]
CWR22R	IC₅₀	46.25 μM Compound: 3	Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay	[PMID: 27301368]
CWR22R	IC₅₀	49.58 μM Compound: 1	Antiproliferative activity against human 22Rv1 cells after 96 hrs by propidium iodide staining-based fluorescence assay Antiproliferative activity against human 22Rv1 cells after 96 hrs by propidium iodide staining-based fluorescence assay	[PMID: 30108852]
CWR22R	IC₅₀	46.3 μM Compound: R-(1)	Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay	[PMID: 31288149]
DU-145	IC₅₀	41.172 μM Compound: 45a; R-Bicalutamide	Antiproliferative activity against human DU145 cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay Antiproliferative activity against human DU145 cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	[PMID: 27131065]
DU-145	IC₅₀	45.41 μM Compound: 45a; R-Bicalutamide	Antiproliferative activity against human DU145 cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay Antiproliferative activity against human DU145 cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	[PMID: 27131065]
DU-145	IC₅₀	45.41 μM Compound: 3	Antiproliferative activity against human DU145 cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay Antiproliferative activity against human DU145 cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay	[PMID: 27301368]
DU-145	IC₅₀	49.2 μM Compound: 1	Antiproliferative activity against human DU145 cells after 96 hrs by propidium iodide staining-based fluorescence assay Antiproliferative activity against human DU145 cells after 96 hrs by propidium iodide staining-based fluorescence assay	[PMID: 30108852]
DU-145	IC₅₀	45.4 μM Compound: R-(1)	Antiproliferative activity against human DU145 cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay Antiproliferative activity against human DU145 cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay	[PMID: 31288149]
HEK293	IC₅₀	0.248 μM Compound: 4	Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of R1881-induced receptor transactivation after 24 hrs by luciferase reporter gene assay Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of R1881-induced receptor transactivation after 24 hrs by luciferase reporter gene assay	[PMID: 30525603]
LNCaP	IC₅₀	8.7 x 10^-7/ M Compound: 5	Growth inhibition of human LNCAP cells after 3 days Growth inhibition of human LNCAP cells after 3 days	[PMID: 20521823]
LNCaP	GI₅₀	1.8 μM Compound: (R)-12a, (R)-Bic	Growth inhibition of human LNCAP cells expressing mutant androgen receptor after 144 hrs by SRB assay Growth inhibition of human LNCAP cells expressing mutant androgen receptor after 144 hrs by SRB assay	[PMID: 25121586]
LNCaP	IC₅₀	0.85 μM Compound: 1	Antagonist activity at AR T877A mutant expressed in human LNCaP cells assessed as inhibition of 10 nM DHT-stimulated cell proliferation after 6 days by WST-8 assay Antagonist activity at AR T877A mutant expressed in human LNCaP cells assessed as inhibition of 10 nM DHT-stimulated cell proliferation after 6 days by WST-8 assay	[PMID: 26295173]
LNCaP	IC₅₀	45.196 μM Compound: 45a; R-Bicalutamide	Antiproliferative activity against human LNCAP cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay Antiproliferative activity against human LNCAP cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	[PMID: 27131065]
LNCaP	IC₅₀	47.002 μM Compound: 45a; R-Bicalutamide	Antiproliferative activity against human LNCAP cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay Antiproliferative activity against human LNCAP cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	[PMID: 27131065]
LNCaP	IC₅₀	45.2 μM Compound: 3	Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay	[PMID: 27301368]
LNCaP	IC₅₀	45.27 μM Compound: 1	Antiproliferative activity against human LNCAP cells after 96 hrs by propidium iodide staining-based fluorescence assay Antiproliferative activity against human LNCAP cells after 96 hrs by propidium iodide staining-based fluorescence assay	[PMID: 30108852]
LNCaP	IC₅₀	20.44 μM Compound: Bical	Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability after 96 hrs by MTT assay Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability after 96 hrs by MTT assay	[PMID: 30743097]
LNCaP	IC₅₀	45.2 μM Compound: R-(1)	Antiproliferative activity against human LNCAP cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay Antiproliferative activity against human LNCAP cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay	[PMID: 31288149]
PC-3	IC₅₀	59.83 μM Compound: R-BIC	Antiproliferative activity against AR negative human PC3 cells after 48 hrs by MTT assay Antiproliferative activity against AR negative human PC3 cells after 48 hrs by MTT assay	[PMID: 28162857]
PC-3	IC₅₀	92.63 μM Compound: Bical	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 96 hrs by MTT assay Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 96 hrs by MTT assay	[PMID: 30743097]
SC-3	IC₅₀	0.27 μM Compound: 6, (R)- bicalutamide (Casodex)	Antagonist activity at wild type human recombinant androgen receptor assessed as inhibition of testosterone-induced growth of mouse androgen dependent SC3 cells by WST-1 method Antagonist activity at wild type human recombinant androgen receptor assessed as inhibition of testosterone-induced growth of mouse androgen dependent SC3 cells by WST-1 method	[PMID: 18571420]
SC-3	IC₅₀	1.4 x 10^-7 M Compound: 5	Growth inhibition of mouse SC3 cells after 3 days by WST-8 assay Growth inhibition of mouse SC3 cells after 3 days by WST-8 assay	[PMID: 20521823]
SC-3	IC₅₀	1.4 x 10^-1 μM Compound: 5	Growth inhibition of mouse SC3 cells after 3 days by WST-8 assay Growth inhibition of mouse SC3 cells after 3 days by WST-8 assay	[PMID: 20521823]
VCaP	IC₅₀	39.793 μM Compound: 45a; R-Bicalutamide	Antiproliferative activity against human VCaP cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay Antiproliferative activity against human VCaP cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	[PMID: 27131065]
VCaP	IC₅₀	51.607 μM Compound: 45a; R-Bicalutamide	Antiproliferative activity against human VCaP cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay Antiproliferative activity against human VCaP cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	[PMID: 27131065]
VCaP	IC₅₀	51.61 μM Compound: 3	Antiproliferative activity against human VCaP cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay Antiproliferative activity against human VCaP cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay	[PMID: 27301368]
VCaP	IC₅₀	68.37 μM Compound: 1	Antiproliferative activity against human VCaP cells after 96 hrs by propidium iodide staining-based fluorescence assay Antiproliferative activity against human VCaP cells after 96 hrs by propidium iodide staining-based fluorescence assay	[PMID: 30108852]
VCaP	IC₅₀	5.96 μM Compound: Bical	Antiproliferative activity against human VCaP cells assessed as reduction in cell viability after 96 hrs by MTS assay Antiproliferative activity against human VCaP cells assessed as reduction in cell viability after 96 hrs by MTS assay	[PMID: 30743097]
VCaP	IC₅₀	51.6 μM Compound: R-(1)	Antiproliferative activity against human VCaP cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay Antiproliferative activity against human VCaP cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay	[PMID: 31288149]

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 na ve LNCaP cells survival in a dose-dependent manner^[2].

MedChemExpress (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 IC₅₀ value of about 7 μM; 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].

MedChemExpress (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.

Chemical Information

No. CAS 113299-40-4
Appearance Solid
Peso molecular 430.37
Fòrmula C₁₈H₁₄F₄N₂O₄S
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (232.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. 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. J Comput Aided Mol Des. 2016 Dec;30(12):1189-1200. [Content Brief]

[2]. Sara Pignatta, et al. Prolonged exposure to (R)-bicalutamide generates a LNCaP subclone with alteration of mitochondrial genome. Mol Cell Endocrinol. 2014 Jan 25;382(1):314-324. [Content Brief]

[3]. Anna Tesei, et al. Effect of Small Molecules Modulating Androgen Receptor (SARMs) in Human Prostate Cancer Models. PLoS One. 2013; 8(5): e62657. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3236 mL	11.6179 mL	23.2358 mL	58.0896 mL
	5 mM	0.4647 mL	2.3236 mL	4.6472 mL	11.6179 mL
	10 mM	0.2324 mL	1.1618 mL	2.3236 mL	5.8090 mL
	15 mM	0.1549 mL	0.7745 mL	1.5491 mL	3.8726 mL
	20 mM	0.1162 mL	0.5809 mL	1.1618 mL	2.9045 mL
	25 mM	0.0929 mL	0.4647 mL	0.9294 mL	2.3236 mL
	30 mM	0.0775 mL	0.3873 mL	0.7745 mL	1.9363 mL
	40 mM	0.0581 mL	0.2904 mL	0.5809 mL	1.4522 mL
	50 mM	0.0465 mL	0.2324 mL	0.4647 mL	1.1618 mL
	60 mM	0.0387 mL	0.1936 mL	0.3873 mL	0.9682 mL
	80 mM	0.0290 mL	0.1452 mL	0.2904 mL	0.7261 mL
	100 mM	0.0232 mL	0.1162 mL	0.2324 mL	0.5809 mL

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(R)-Bicalutamide

Anti-Cancer Compound Library

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Transcription Factor-Targeted Library

Anti-Prostate Cancer Compound Library

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Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

(R)-Bicalutamide

Anti-Cancer Compound Library

Orally Active Compound Library

Transcription Factor-Targeted Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

(R)-Bicalutamide Related Classifications

HY-108250 Related Classifications