Flutamide (Synonyms: 氟他胺; SCH 13521)

目录号: HY-B0022 纯度: 99.90%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Flutamide 是雄激素受体 (Androgen Receptor) 拮抗剂，Ki=55 nM。Flutamide 可抑制前列腺癌发展，并与 Docetaxel (HY-B0011) 具有协同增效作用。Flutamide 还有潜力防止高温引起的多器官功能障碍综合征。

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Flutamide Chemical Structure

CAS No. : 13311-84-7

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥500	In-stock
500 mg	￥281	In-stock
1 g	￥400	In-stock
5 g		询价
10 g		询价

or 大包装询价

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Other Forms of Flutamide:

Flutamide (Standard) In-stock
Flutamide-d₇ 询价

MCE 顾客使用本产品发表的 6 篇科研文献

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生物活性
纯度 & 产品资料
参考文献

生物活性

Flutamide is an Androgen Receptor antagonist with Ki=55 nM. Flutamide inhibits prostate cancer progression and has synergistic effects with Docetaxel (HY-B0011). Flutamide also has the potential to protect against hyperthermia-induced multiple organ dysfunction syndrome^[1]^[2]^[3]^[4]^[5]^[6]^[7].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
COS-7	IC₅₀	51.51 μM Compound: Flutamide	Anticancer activity against African green monkey COS7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Anticancer activity against African green monkey COS7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 32866675]
CV-1	IC₅₀	110 μM Compound: flutamide	Antagonist activity at human androgen receptor expressed in human CV1 cells assessed as inhibition of receptor-mediated transactivation by MMTV-luciferase reporter gene assay Antagonist activity at human androgen receptor expressed in human CV1 cells assessed as inhibition of receptor-mediated transactivation by MMTV-luciferase reporter gene assay	[PMID: 20826091]
HCT-15	IC₅₀	> 100 μM Compound: Flutamide	Anticancer activity against human HCT-15 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Anticancer activity against human HCT-15 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 32866675]
K562	IC₅₀	29.2 μM Compound: Flutamide	Anticancer activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Anticancer activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 32866675]
LNCaP	IC₅₀	0.9 μM Compound: Flutamide	Anticancer activity against human LNCAP cells after 24 hrs by MTT assay in presence of testosterone Anticancer activity against human LNCAP cells after 24 hrs by MTT assay in presence of testosterone	[PMID: 21600678]
LNCaP	IC₅₀	47.55 μM Compound: Flutamide	Cytotoxicity against human LNCAP cells after 48 hrs by MTT assay Cytotoxicity against human LNCAP cells after 48 hrs by MTT assay	[PMID: 28757062]
LNCaP	EC₅₀	7 μM Compound: Flutamide	Cytotoxicity against human LNCAP cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against human LNCAP cells assessed as reduction in cell viability after 24 hrs by MTT assay	10.1039/C6MD00426A
LNCaP	EC₅₀	7 μM Compound: Flutamide	Cytotoxicity against human LNCAP cells after 24 hrs by MTT assay Cytotoxicity against human LNCAP cells after 24 hrs by MTT assay	[PMID: 28363155]
LNCaP	IC₅₀	81.8 μM Compound: Flutamide	Cytotoxicity against androgen-dependent human LNCAP cells after 72 hrs by SRB assay Cytotoxicity against androgen-dependent human LNCAP cells after 72 hrs by SRB assay	[PMID: 22672984]
MDA-MB-453	IC₅₀	2 μM Compound: Flutamide	Antiandrogenic activity in human MDA-MB-453 cells expressing androgen receptor assessed as inhibition of DHT-induced androgen-dependent transcription by luciferase reporter gene assay Antiandrogenic activity in human MDA-MB-453 cells expressing androgen receptor assessed as inhibition of DHT-induced androgen-dependent transcription by luciferase reporter gene assay	[PMID: 19131248]
NCI-H1299	IC₅₀	> 500 μM Compound: Flutamide	Anticancer activity against human H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Anticancer activity against human H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34425478]
NIH3T3	IC₅₀	5.8 x 10^-1 μM Compound: 1a, flu	Antagonist activity at human androgen receptor expressed in mouse NIH3T3 cells assessed as inhibition of DHT-induced transcriptional activation after 24 hrs by androgen response element-mediated luciferase reporter gene assay Antagonist activity at human androgen receptor expressed in mouse NIH3T3 cells assessed as inhibition of DHT-induced transcriptional activation after 24 hrs by androgen response element-mediated luciferase reporter gene assay	[PMID: 18707892]
PC-3	IC₅₀	20.3 μM Compound: Flutamide	Anticancer activity against human PC-3 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Anticancer activity against human PC-3 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 32866675]
PC-3	IC₅₀	58 μM Compound: Flutamide	Anticancer activity against human PC-3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Anticancer activity against human PC-3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34425478]
PC-3	IC₅₀	67.34 μM Compound: Flutamide	Cytotoxicity against human PC3 cells after 48 hrs by MTT assay Cytotoxicity against human PC3 cells after 48 hrs by MTT assay	[PMID: 28757062]
PC-3	IC₅₀	98.8 μM Compound: Flutamide	Cytotoxicity against androgen-independent human PC3 cells after 72 hrs by SRB assay Cytotoxicity against androgen-independent human PC3 cells after 72 hrs by SRB assay	[PMID: 22672984]
SC-3	IC₅₀	4.2 μM Compound: 4, flutamide	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	7.2 x 10^-1 μM Compound: 3	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]
U-251	IC₅₀	22.11 μM Compound: Flutamide	Anticancer activity against human U-251 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Anticancer activity against human U-251 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 32866675]

体外研究
(In Vitro)

Flutamide 的活性代谢物是 Flutamide-OH。两者均直接结合大鼠垂体前叶雄激素受体(Ki=55 nM)^[1]。
Flutamide 不影响培养的小鼠乳腺癌Shionogi SC-l 15细胞的雄激素敏感克隆的增殖，仅显示抗雄激素作用，但不显示雄激素作用^[2]。
Flutamide 与 Leuprolides 一起使用可抑制前列腺癌^[3]。
Flutamide 对 PC3 和 LNCap 具有细胞毒活性 (IC50s 分别为 20 μM 和 12 μM)。Flutamide (10 μM, 5 μM; 48 h) 诱导 PC3 和 LNCap 细胞凋亡，减少细胞迁移和定植^[4]。
Flutamide 还下调细胞中 KLK2 和 EMT 通路基因的表达^[4]。

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

体内研究
(In Vivo)

Flutamide 导致大鼠腹侧前列腺重量从 319 mg 显着减少至 245 mg。Flutamide 和 LHRH 激动剂的组合可产生叠加效应，前列腺重量降至 101 mg，前列腺 ODC 活性显着下降^[5]。
Flutamide (12.5-50 mg/kg；皮下注射；每天一次，连续 3 天) 缓解热应激小鼠的中暑^[6]。

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

Clinical Trial

分子量

276.21

Formula

C₁₁H₁₁F₃N₂O₃

CAS 号

13311-84-7

性状

固体

颜色

Light yellow to yellow

中文名称

氟他胺

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (362.04 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.6204 mL	18.1022 mL	36.2043 mL
5 mM	0.7241 mL	3.6204 mL	7.2409 mL
10 mM	0.3620 mL	1.8102 mL	3.6204 mL

查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.05 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.05 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (9.05 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.90%

选择批次：

Data Sheet (647 KB) SDS (418 KB)

COA (192 KB) LCMS (92 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Simard J, et al. Characteristics of interaction of the antiandrogen flutamide with the androgen receptor in various target tissues. Mol Cell Endocrinol. 1986 Mar;44(3):261-70. [Content Brief]

[2]. Luthy IA, et al. Androgenic activity of synthetic progestins and spironolactone in androgen-sensitive mouse mammary carcinoma (Shionogi) cells in culture. J Steroid Biochem. 1988 Nov;31(5):845-52. [Content Brief]

[3]. Crawford ED, et al. A controlled trial of leuprolide with and without flutamide in prostatic carcinoma. N Engl J Med. 1989 Aug 17;321(7):419-24. [Content Brief]

[4]. Rahimnia R, et al. The effect of Ganoderma lucidum polysaccharide extract on sensitizing prostate cancer cells to flutamide and docetaxel: an in vitro study. Sci Rep. 2023 Nov 2;13(1):18940. [Content Brief]

[5]. Lin CY, et al. Flutamide, an androgen receptor antagonist, improves heatstroke outcomes in mice. Eur J Pharmacol. 2012 Aug 5;688(1-3):62-7. [Content Brief]

[6]. Marchetti B, et al. Characteristics of flutamide action on prostatic and testicular functions in the rat. J Steroid Biochem. 1988 Jun;29(6):691-8. [Content Brief]

Flutamide 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.6204 mL	18.1022 mL	36.2043 mL	90.5108 mL
	5 mM	0.7241 mL	3.6204 mL	7.2409 mL	18.1022 mL
	10 mM	0.3620 mL	1.8102 mL	3.6204 mL	9.0511 mL
	15 mM	0.2414 mL	1.2068 mL	2.4136 mL	6.0341 mL
	20 mM	0.1810 mL	0.9051 mL	1.8102 mL	4.5255 mL
	25 mM	0.1448 mL	0.7241 mL	1.4482 mL	3.6204 mL
	30 mM	0.1207 mL	0.6034 mL	1.2068 mL	3.0170 mL
	40 mM	0.0905 mL	0.4526 mL	0.9051 mL	2.2628 mL
	50 mM	0.0724 mL	0.3620 mL	0.7241 mL	1.8102 mL
	60 mM	0.0603 mL	0.3017 mL	0.6034 mL	1.5085 mL
	80 mM	0.0453 mL	0.2263 mL	0.4526 mL	1.1314 mL
	100 mM	0.0362 mL	0.1810 mL	0.3620 mL	0.9051 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Flutamide13311-84-7SCH 13521氟他胺SCH13521SCH-13521Androgen ReceptorInhibitorinhibitorinhibit

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Flutamide (Synonyms: 氟他胺; SCH 13521)

Customer Review

Other Forms of Flutamide:

MCE 顾客使用本产品发表的 6 篇科研文献

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Flutamide (Synonyms: 氟他胺; SCH 13521)

Customer Review

Other Forms of Flutamide:

Flutamide 相关抗体

MCE 顾客使用本产品发表的 6 篇科研文献

Flutamide 相关产品

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•同靶点产品:

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参考文献

Flutamide 相关抗体:

摩尔计算器

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完整储备液配制表

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