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  1. Vitamin D Related/Nuclear Receptor
  2. Androgen Receptor
  3. Flutamide

Flutamide  (Synonyms: 氟他胺; SCH 13521)

目錄號(hào): HY-B0022 純度: 99.90%
COA 產(chǎn)品使用指南 技術(shù)支持

Flutamide 是雄激素受體 (Androgen Receptor) 拮抗劑,Ki=55 nM。Flutamide 可抑制前列腺癌發(fā)展,并與 Docetaxel (HY-B0011) 具有協(xié)同增效作用。Flutamide 還有潛力防止高溫引起的多器官功能障礙綜合征。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào),我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Flutamide Chemical Structure

Flutamide Chemical Structure

CAS No. : 13311-84-7

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10 mM * 1 mL in DMSO ¥500
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1 g ¥400
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Other Forms of Flutamide:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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].

細(xì)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]
體外研究
(In Vitro)

Flutamide 的活性代謝物是 Flutamide-OH。 兩者均直接結(jié)合大鼠垂體前葉雄激素受體(Ki=55 nM)[1]。
Flutamide 不影響培養(yǎng)的小鼠乳腺癌Shionogi SC-l 15細(xì)胞的雄激素敏感克隆的增殖,僅顯示抗雄激素作用,但不顯示雄激素作用[2]。
Flutamide 與 Leuprolides 一起使用可抑制前列腺癌[3]。
Flutamide 對(duì) PC3 和 LNCap 具有細(xì)胞毒活性 (IC50s 分別為 20 μM 和 12 μM)。Flutamide (10 μM, 5 μM; 48 h) 誘導(dǎo) PC3 和 LNCap 細(xì)胞凋亡,減少細(xì)胞遷移和定植[4]。
Flutamide 還下調(diào)細(xì)胞中 KLK2 和 EMT 通路基因的表達(dá)[4]

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

體內(nèi)研究
(In Vivo)

Flutamide 導(dǎo)致大鼠腹側(cè)前列腺重量從 319 mg 顯著減少至 245 mg。Flutamide 和 LHRH 激動(dòng)劑的組合可產(chǎn)生疊加效應(yīng),前列腺重量降至 101 mg,前列腺 ODC 活性顯著下降[5]。
Flutamide (12.5-50 mg/kg;皮下注射;每天一次,連續(xù) 3 天) 緩解熱應(yīng)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 號(hào)
性狀

固體

顏色

Light yellow to yellow

中文名稱

氟他胺

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 100 mg/mL (362.04 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn):

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.05 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.05 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

    2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上,請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.90%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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.

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產(chǎn)品名稱:
Flutamide
目錄號(hào):
HY-B0022
需求量: