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  2. Metabolic Enzyme/Protease Autophagy
  3. Cytochrome P450 Autophagy
  4. Letrozole

Letrozole  (Synonyms: 來曲唑; CGS 20267)

目錄號(hào): HY-14248 純度: 99.95%
COA 產(chǎn)品使用指南

Letrozole (CGS 20267) 是一種有效的，選擇性的，可逆的和具有口服活性的非甾體類芳香化酶 (aromatase) 抑制劑，IC50 值為 11.5 nM。Letrozole 選擇性抑制雌激素的生物合成，可用于乳腺癌的研究。

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)

Letrozole Chemical Structure

Letrozole Chemical Structure

CAS No. : 112809-51-5

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥715
In-stock
25 mg ￥650
In-stock
50 mg ￥900
In-stock
100 mg ￥1600
In-stock
200 mg ￥2800
In-stock
500 mg ￥4100
In-stock
1 g   詢價(jià)  
5 g   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Letrozole:

    Letrozole purchased from MCE. Usage Cited in: Exp Ther Med. 2018 Jun;15(6):5269-5274.  [Abstract]

    Letrozole significantly increases the protein levels of Ras/ERK1/c-Myc in the classical MAPK pathway.

    Letrozole purchased from MCE. Usage Cited in: Exp Ther Med. 2018 Jun;15(6):5269-5274.  [Abstract]

    Detection of the effects of Letrozole and the MAPK pathway on the proliferation of GC-1 spg cells by BrdU. MAPK, mitogen-activated protein kinase; spg, spermatogonia; BrdU, bromodeoxyuridine.

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer[1][2][3].

    IC50 & Target

    Aromatase

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    BT-549 GI50
    0.89 μM
    Compound: Letrozole
    Growth inhibition of human BT549 cells after 48 hrs by sulforhodamine B assay
    Growth inhibition of human BT549 cells after 48 hrs by sulforhodamine B assay
    		[PMID: 20950898]
    HeLa GI50
    > 100 μM
    Compound: Letrozole
    Growth inhibition of non-estrogen-sensitive human HeLa cells after 72 hrs by MTT assay
    Growth inhibition of non-estrogen-sensitive human HeLa cells after 72 hrs by MTT assay
    		[PMID: 24025069]
    Hs-578T GI50
    2.17 μM
    Compound: Letrozole
    Growth inhibition of human Hs 578T cells after 48 hrs by sulforhodamine B assay
    Growth inhibition of human Hs 578T cells after 48 hrs by sulforhodamine B assay
    		[PMID: 20950898]
    HT-29 GI50
    > 100 μM
    Compound: Letrozole
    Growth inhibition of non-estrogen-sensitive human HT-29 cells after 72 hrs by MTT assay
    Growth inhibition of non-estrogen-sensitive human HT-29 cells after 72 hrs by MTT assay
    		[PMID: 24025069]
    IGROV-1 GI50
    > 100 μM
    Compound: Letrozole
    Growth inhibition of estrogen-sensitive human IGROV1 cells after 72 hrs by MTT assay
    Growth inhibition of estrogen-sensitive human IGROV1 cells after 72 hrs by MTT assay
    		[PMID: 24025069]
    IGROV-1 GI50
    0.095 μM
    Compound: Letrozole
    Growth inhibition of human IGROV1 cells after 48 hrs by sulforhodamine B assay
    Growth inhibition of human IGROV1 cells after 48 hrs by sulforhodamine B assay
    		[PMID: 20950898]
    JEG-3 IC50
    0.89 nM
    Compound: letrozole
    Inhibition of aromatase in human JEG3 cells by scintillation spectrometry
    Inhibition of aromatase in human JEG3 cells by scintillation spectrometry
    		[PMID: 20148564]
    Jurkat GI50
    > 100 μM
    Compound: Letrozole
    Growth inhibition of non-estrogen-sensitive human Jurkat cells after 72 hrs by MTT assay
    Growth inhibition of non-estrogen-sensitive human Jurkat cells after 72 hrs by MTT assay
    		[PMID: 24025069]
    MCF-10A IC50
    > 10 μM
    Compound: Letrozole
    Antiproliferative activity against human MCF-10A cells assessed as reduction in cell viability after 72 hrs by cell counter method
    Antiproliferative activity against human MCF-10A cells assessed as reduction in cell viability after 72 hrs by cell counter method
    		[PMID: 34364162]
    MCF7 GI50
    > 100 μM
    Compound: Letrozole
    Growth inhibition of estrogen-sensitive human MCF7 cells after 72 hrs by MTT assay
    Growth inhibition of estrogen-sensitive human MCF7 cells after 72 hrs by MTT assay
    		[PMID: 24025069]
    MCF7 GI50
    0.7 μM
    Compound: Letrozole
    Growth inhibition of human MCF7 cells after 48 hrs by sulforhodamine B assay
    Growth inhibition of human MCF7 cells after 48 hrs by sulforhodamine B assay
    		[PMID: 20950898]
    MCF7 IC50
    20 nM
    Compound: Letrozole
    Cytotoxicity against human MCF7 cells after 24 to 96 hrs
    Cytotoxicity against human MCF7 cells after 24 to 96 hrs
    		[PMID: 24345481]
    MCF7 IC50
    4.1 μM
    Compound: Letrozole
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by cell counter method
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by cell counter method
    		[PMID: 34364162]
    MCF7 GI50
    4.1 μM
    Compound: LTZ
    Growth inhibition of human MCF7 cells incubated for 72 hrs by cell counting based method
    Growth inhibition of human MCF7 cells incubated for 72 hrs by cell counting based method
    		[PMID: 30822713]
    MCF7 IC50
    4.73 μM
    Compound: Letrozole
    Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
    Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
    		[PMID: 29202405]
    MCF7 IC50
    7 nM
    Compound: Letrozole
    Cytotoxicity against estrogen-dependent human MCF7 cells after 72 hrs by MTT assay
    Cytotoxicity against estrogen-dependent human MCF7 cells after 72 hrs by MTT assay
    		[PMID: 24345481]
    MDA-MB-231 GI50
    0.15 μM
    Compound: Letrozole
    Growth inhibition of human MDA-MB-231cells after 48 hrs by sulforhodamine B assay
    Growth inhibition of human MDA-MB-231cells after 48 hrs by sulforhodamine B assay
    		[PMID: 20950898]
    MDA-MB-231 GI50
    10 μM
    Compound: LTZ
    Growth inhibition of human MDA-MB-231 cells incubated for 72 hrs by cell counting based method
    Growth inhibition of human MDA-MB-231 cells incubated for 72 hrs by cell counting based method
    		[PMID: 30822713]
    MDA-MB-231 GI50
    34 μM
    Compound: LTZ
    Growth inhibition of human ER-negative MDA-MB-231 cells incubated for 72 hrs by cell counter method
    Growth inhibition of human ER-negative MDA-MB-231 cells incubated for 72 hrs by cell counter method
    		[PMID: 32435378]
    MDA-MB-435 GI50
    0.067 μM
    Compound: Letrozole
    Growth inhibition of human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay
    Growth inhibition of human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay
    		[PMID: 20950898]
    MDA-N GI50
    1.61 μM
    Compound: Letrozole
    Growth inhibition of human MDA-N cells after 48 hrs by sulforhodamine B assay
    Growth inhibition of human MDA-N cells after 48 hrs by sulforhodamine B assay
    		[PMID: 20950898]
    NCI/ADR-RES GI50
    1.16 μM
    Compound: Letrozole
    Growth inhibition of human NCI/ADR-RES cells after 48 hrs by sulforhodamine B assay
    Growth inhibition of human NCI/ADR-RES cells after 48 hrs by sulforhodamine B assay
    		[PMID: 20950898]
    NCI-H295R GI50
    > 100 μM
    Compound: Letrozole
    Growth inhibition of estrogen-sensitive human NCI-H295R cells after 72 hrs by MTT assay
    Growth inhibition of estrogen-sensitive human NCI-H295R cells after 72 hrs by MTT assay
    		[PMID: 24025069]
    OVCAR-3 GI50
    > 100 μM
    Compound: Letrozole
    Growth inhibition of estrogen-sensitive human OVCAR3 cells after 72 hrs by MTT assay
    Growth inhibition of estrogen-sensitive human OVCAR3 cells after 72 hrs by MTT assay
    		[PMID: 24025069]
    OVCAR-3 GI50
    5.87 μM
    Compound: Letrozole
    Growth inhibition of human OVCAR3 cells after 48 hrs by sulforhodamine B assay
    Growth inhibition of human OVCAR3 cells after 48 hrs by sulforhodamine B assay
    		[PMID: 20950898]
    OVCAR-4 GI50
    0.88 μM
    Compound: Letrozole
    Growth inhibition of human OVCAR4 cells after 48 hrs by sulforhodamine B assay
    Growth inhibition of human OVCAR4 cells after 48 hrs by sulforhodamine B assay
    		[PMID: 20950898]
    OVCAR-5 GI50
    1.62 μM
    Compound: Letrozole
    Growth inhibition of human OVCAR5 cells after 48 hrs by sulforhodamine B assay
    Growth inhibition of human OVCAR5 cells after 48 hrs by sulforhodamine B assay
    		[PMID: 20950898]
    OVCAR-8 GI50
    4.5 μM
    Compound: Letrozole
    Growth inhibition of human OVCAR8 cells after 48 hrs by sulforhodamine B assay
    Growth inhibition of human OVCAR8 cells after 48 hrs by sulforhodamine B assay
    		[PMID: 20950898]
    RS4-11 GI50
    > 100 μM
    Compound: Letrozole
    Growth inhibition of non-estrogen-sensitive human RS4:11 cells after 72 hrs by MTT assay
    Growth inhibition of non-estrogen-sensitive human RS4:11 cells after 72 hrs by MTT assay
    		[PMID: 24025069]
    SEM GI50
    > 100 μM
    Compound: Letrozole
    Growth inhibition of non-estrogen-sensitive human SEM cells after 72 hrs by MTT assay
    Growth inhibition of non-estrogen-sensitive human SEM cells after 72 hrs by MTT assay
    		[PMID: 24025069]
    SK-OV-3 GI50
    1.09 μM
    Compound: Letrozole
    Growth inhibition of human SKOV3 cells after 48 hrs by sulforhodamine B assay
    Growth inhibition of human SKOV3 cells after 48 hrs by sulforhodamine B assay
    		[PMID: 20950898]
    T47D GI50
    0.44 μM
    Compound: Letrozole
    Growth inhibition of human T47D cells after 48 hrs by sulforhodamine B assay
    Growth inhibition of human T47D cells after 48 hrs by sulforhodamine B assay
    		[PMID: 20950898]
    T47D IC50
    29.5 μM
    Compound: Letrozole
    Inhibition of aromatase activity in human T47D cells after 24 hrs
    Inhibition of aromatase activity in human T47D cells after 24 hrs
    		[PMID: 27770735]
    體外研究
    (In Vitro)

    Letrozole（0.1-100 nM；24-96 小時(shí)）以劑量和時(shí)間依賴性方式顯著抑制 MCF-7 上皮性乳腺癌細(xì)胞的生長(zhǎng)[2]。
    Letrozole (10 nM) 顯著抑制睪酮對(duì) MCF-7 細(xì)胞增殖的刺激作用[2]。
    Letrozole（10 nM；24-48 小時(shí)）可抑制 MCF-7 細(xì)胞中分泌的金屬蛋白酶（MMP-2 和 MMP-9）的水平[2]。

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

    Cell Viability Assay[2]

    Cell Line: MCF-7 cells
    Concentration: 0.1, 1, 10, 100 nM
    Incubation Time: 24, 48, 96 hours
    Result: Inhibited cells growth in a dose- and time-dependent manner.
    體內(nèi)研究
    (In Vivo)

    Letrozole（3-300 μg/kg；口服管飼，每天一次，持續(xù) 6 周）在大鼠中表現(xiàn)出抗腫瘤作用[3]。

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

    Animal Model: Adult female rats bearing mammary tumors[3]
    Dosage: 3, 10, 30, 100, 300 μg/kg
    Administration: Oral gavage once daily for 6 weeks
    Result: Induced complete regression of mammary tumors, with an ED50 of 10-30 μg/kg/day.
    Clinical Trial
    分子量

    285.30

    Formula

    C17H11N5
    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    來曲唑
    結(jié)構(gòu)分類
    初始來源
    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 : 50 mg/mL (175.25 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)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 3.5051 mL 17.5254 mL 35.0508 mL
    5 mM 0.7010 mL 3.5051 mL 7.0102 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: ≥ 2.08 mg/mL (7.29 mM); 澄清溶液

      此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (7.29 mM); 澄清溶液

      此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 20.8 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

    只
    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(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
    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(guó)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: 99.95%

    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 3.5051 mL 17.5254 mL 35.0508 mL 87.6271 mL
    5 mM 0.7010 mL 3.5051 mL 7.0102 mL 17.5254 mL
    10 mM 0.3505 mL 1.7525 mL 3.5051 mL 8.7627 mL
    15 mM 0.2337 mL 1.1684 mL 2.3367 mL 5.8418 mL
    20 mM 0.1753 mL 0.8763 mL 1.7525 mL 4.3814 mL
    25 mM 0.1402 mL 0.7010 mL 1.4020 mL 3.5051 mL
    30 mM 0.1168 mL 0.5842 mL 1.1684 mL 2.9209 mL
    40 mM 0.0876 mL 0.4381 mL 0.8763 mL 2.1907 mL
    50 mM 0.0701 mL 0.3505 mL 0.7010 mL 1.7525 mL
    60 mM 0.0584 mL 0.2921 mL 0.5842 mL 1.4605 mL
    80 mM 0.0438 mL 0.2191 mL 0.4381 mL 1.0953 mL
    100 mM 0.0351 mL 0.1753 mL 0.3505 mL 0.8763 mL
    Help & FAQs
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    產(chǎn)品名稱：
    Letrozole
    目錄號(hào)：
    HY-14248
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