(R)-Bicalutamide-武汉科斯坦生物科技有限公司

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(R)-Bicalutamide

英文名称：(R)-Bicalutamide

品牌：Chemstan

产地：中国

货号：CS-108250

cas：113299-40-4

价格： ￥1500/mg
发布日期： 2021-03-10
更新日期： 2025-11-10

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产地	中国
品牌	Chemstan
货号	CS-108250
用途	科研
英文名称	(R)-Bicalutamide
包装规格	5 mg
纯度	98.00%%
CAS编号	113299-40-4
别名
分子式
是否进口	否

Description

(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^[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 na?ve 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 na?ve 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

C??H??F?N?O?S

CAS No.

113299-40-4

中文名称

(R)-比卡鲁胺

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

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

ConcentrationSolventMass	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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (5.81 mM); Clear solution
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.81 mM); Clear solution
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

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

*以上所有助溶剂都可在 MCE 网站选购。

References

[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.

[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.

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