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  2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Autophagy
  3. RAR/RXR Autophagy
  4. Bexarotene

Bexarotene  (Synonyms: 貝沙羅汀; LGD1069)

目錄號: HY-14171 純度: 99.92%
COA 產(chǎn)品使用指南 技術(shù)支持

Bexarotene (LGD1069) 是一種高親和力的選擇性類視黃醇 X 受體 (RXR) 激動劑，對 RXRα、RXRβ 和 RXRγ 的 EC50 分別為 33、24、25 nM。Bexarotene 對 RAR 受體的親和力有限 (EC50 >10000 nM)。Bexarotene 可用于皮膚 T 細胞淋巴瘤的研究。

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

Bexarotene Chemical Structure

Bexarotene Chemical Structure

CAS No. : 153559-49-0

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥366
In-stock
10 mg ￥333
In-stock
25 mg ￥535
In-stock
50 mg ￥736
In-stock
100 mg ￥1056
In-stock
200 mg ￥1480
In-stock
500 mg ￥2963
In-stock
1 g   詢價  
5 g   詢價  

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Customer Review

Other Forms of Bexarotene:

    Bexarotene purchased from MCE. Usage Cited in: Neurobiol Dis. 2018 Sep;117:114-124.  [Abstract]

    Bexarotene increases neuronal maintenance and inhibits cell apoptosis after controlled cortical impact (CCI). Representative Western blotting images of cleaved caspase-3, Bax and Bcl-2 in ipsilateral brain on the 14th day after CCI.

    Bexarotene purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2016;40(5):1239-1251.  [Abstract]

    Arithmetic means±SEM (n=14) of erythrocyte annexin-V-binding following incubation for 48 hours to Ringer solution without (white bar) or with (black bars) bexarotene (0.2-0.6 μg/mL). For comparison, the effect of the solvent DMSO is shown (grey bar).

    查看 RAR/RXR 亞型特異性產(chǎn)品:

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

    Bexarotene?(LGD1069) is a high-affinity and selective?retinoid X receptors (RXR)?agonist with EC50s?of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50?>10000 nM)[1][2][3]. Bexarotene can be used for the research of cutaneous T-cell lymphoma.

    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A2780 IC50
    26.5 μM
    Compound: Bexarotene
    Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
    Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
    		[PMID: 32422522]
    A-375 IC50
    28.4 μM
    Compound: Bexarotene
    Cytotoxicity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
    Cytotoxicity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
    		[PMID: 32422522]
    BT-549 EC50
    > 56 μM
    Compound: Bex
    Cytotoxicity against human BT549 cells assessed as reduction in cell viability by MTT assay
    Cytotoxicity against human BT549 cells assessed as reduction in cell viability by MTT assay
    		[PMID: 29287960]
    Caco-2 EC50
    52 nM
    Compound: 1, Bexarotene
    Agonist activity at human recombinant Gal4-tagged RXRalpha expressed in human Caco-2 cells assessed as receptor homodimerization after 24 hrs by mammalian two hybrid assay
    Agonist activity at human recombinant Gal4-tagged RXRalpha expressed in human Caco-2 cells assessed as receptor homodimerization after 24 hrs by mammalian two hybrid assay
    		[PMID: 19791803]
    COS-1 EC50
    20 nM
    Compound: Bexarotene
    Agonist activity at RXRalpha (unknown origin) expressed in COS1 cells incubated for 18 hrs by luciferase reporter gene assay
    Agonist activity at RXRalpha (unknown origin) expressed in COS1 cells incubated for 18 hrs by luciferase reporter gene assay
    		[PMID: 25815156]
    COS-1 EC50
    20 nM
    Compound: 1, LGD1069
    Agonist activity at RXRalpha transfected in human COS1 cells after 18 hrs by luciferase reporter gene transactivation assay
    Agonist activity at RXRalpha transfected in human COS1 cells after 18 hrs by luciferase reporter gene transactivation assay
    		[PMID: 24900241]
    CV-1 EC50
    0.04 μM
    Compound: 37, LGD1069
    Transactivation of Gal4-LBD fused mouse RXRalpha (218 to 467) transfected in african green monkey CV1 cells assessed as luciferase activity at after 6 hrs by Dual-light chemiluminescent assay
    Transactivation of Gal4-LBD fused mouse RXRalpha (218 to 467) transfected in african green monkey CV1 cells assessed as luciferase activity at after 6 hrs by Dual-light chemiluminescent assay
    		[PMID: 19216008]
    DU-145 IC50
    61.6 μM
    Compound: bexarotene
    Cytotoxicity against human DU145 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human DU145 cells assessed as growth inhibition after 72 hrs by MTT assay
    		[PMID: 23707260]
    FaDu IC50
    29.8 μM
    Compound: Bexarotene
    Cytotoxicity against human FaDu cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
    Cytotoxicity against human FaDu cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
    		[PMID: 32422522]
    HEK293 EC50
    149 nM
    Compound: bexarotene
    Transactivation of human RXRalpha transfected in human 293 cells after 48 hrs by dual-luciferase reporter gene assay
    Transactivation of human RXRalpha transfected in human 293 cells after 48 hrs by dual-luciferase reporter gene assay
    		[PMID: 23707260]
    HEK293 EC50
    40 nM
    Compound: Targretin, Bexarotene
    Agonist activity at Gal4-fused human RXR-alpha expressed in HEK293 cells assessed as receptor-mediated transcriptional activity treated 24 hrs after transfection measured 48 hrs post-transfection by dual luciferase reporter assay
    Agonist activity at Gal4-fused human RXR-alpha expressed in HEK293 cells assessed as receptor-mediated transcriptional activity treated 24 hrs after transfection measured 48 hrs post-transfection by dual luciferase reporter assay
    		[PMID: 24801499]
    HEK-293T EC50
    0.196 μM
    Compound: 18
    Partial agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay
    Partial agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay
    		[PMID: 28169169]
    HEK-293T EC50
    0.434 μM
    Compound: 18
    Partial agonist activity at recombinant human GAL4-DBD-fused LXRbeta-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay
    Partial agonist activity at recombinant human GAL4-DBD-fused LXRbeta-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay
    		[PMID: 28169169]
    Hep 3B2 IC50
    191.8 μM
    Compound: bexarotene
    Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by MTT assay
    		[PMID: 23707260]
    HepG2 IC50
    20 μM
    Compound: 2
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by WST-1 assay
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by WST-1 assay
    		[PMID: 33793232]
    HGC-27 IC50
    32.7 μM
    Compound: bexarotene
    Cytotoxicity against human HGC27 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human HGC27 cells assessed as growth inhibition after 72 hrs by MTT assay
    		[PMID: 23707260]
    HT-29 IC50
    > 30 μM
    Compound: Bexarotene
    Cytotoxicity against human HT29 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
    Cytotoxicity against human HT29 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
    		[PMID: 32422522]
    KB IC50
    46.3 μM
    Compound: bexarotene
    Cytotoxicity against bexarotene-resistant human KB cells assessed as growth inhibition after 48 hrs by MTT assay
    Cytotoxicity against bexarotene-resistant human KB cells assessed as growth inhibition after 48 hrs by MTT assay
    		[PMID: 23707260]
    KB IC50
    8.8 μM
    Compound: bexarotene
    Cytotoxicity against human KB cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human KB cells assessed as growth inhibition after 72 hrs by MTT assay
    		[PMID: 23707260]
    MCF7 IC50
    10.6 μM
    Compound: Bexarotene
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
    		[PMID: 32422522]
    MDA-MB-231 EC50
    > 56 μM
    Compound: Bex
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability by MTT assay
    		[PMID: 29287960]
    NIH3T3 IC50
    18.7 μM
    Compound: Bexarotene
    Cytotoxicity against mouse NIH3T3 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
    Cytotoxicity against mouse NIH3T3 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
    		[PMID: 32422522]
    Sf9 IC50
    13.5 μM
    Compound: 40
    Inhibition of microsomal fraction of human CYP26A1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 1 min by HPLC analysis in presence of rat P450 reductase
    Inhibition of microsomal fraction of human CYP26A1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 1 min by HPLC analysis in presence of rat P450 reductase
    		[PMID: 26918322]
    Sf9 IC50
    5.9 μM
    Compound: 40
    Inhibition of microsomal fraction of human CYP26B1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins by HPLC analysis in presence of rat P450 reductase
    Inhibition of microsomal fraction of human CYP26B1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins by HPLC analysis in presence of rat P450 reductase
    		[PMID: 26918322]
    體外研究
    (In Vitro)

    Bexarotene 選擇性結(jié)合并激活 RXR 亞型，對于 RXRα、RXRβ 和 RXRγ 亞型，Kd=14±2 nM、21±4 nM 和 29±7 nM[1]。
    Bexarotene 可有效限制白血病 (HL-60) 細胞的增殖。Bexarotene 在 1 μM 時抑制 HL-60 細胞增殖 37%[1]。
    Bexarotene 單藥處理細胞在高劑量下顯示出抗增殖作用，IC50分別為40.62±0.45 μM (PC3) 和50.20±4.10 μM (DU145)[2]。
    Bexarotene (20 和 40 μM) 和 Docetaxel (5 和 10 μM) 對 PC3 和 DU145 細胞增殖的抑制具有協(xié)同作用[2]。
    Bexarotene (20和 40 μM) 抑制 PC3 和 DU145 細胞中的細胞周期蛋白 D1 和細胞周期蛋白 D3 的表達[2]。

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

    Cell Proliferation Assay[2]

    Cell Line: The human PCa androgen-independent cell lines PC3 and DU145
    Concentration: 5, 10, 20, 30, 40 μM for PC3 cells; 1, 5, 10, 20, 40 μM for DU145 cells.
    Incubation Time: 24 and 48?hours
    Result: Showed an antiproliferative effect with the IC50s were 40.62±0.45?μM (PC3) and 50.20±4.10?μM (DU145).?

    Cell Viability Assay[2]

    Cell Line: PC3 and DU145 cells
    Concentration: 20 and 40?μM
    Incubation Time: 24 or 48?hours
    Result: Decreased cyclin D1, and cyclin E2 after 24?hours treatment.?
    Not only decreased the expression of cyclin D1 and cyclin E2 but repressed cyclin B1 and CDK1 expression after 48?hours treatment.
    體內(nèi)研究
    (In Vivo)

    Bexarotene (1 mg/kg/day) 可有效阻止帕金森病 (PD) 大鼠模型中行為缺陷和多巴胺神經(jīng)元變性的發(fā)展，從而顯著降低甘油三酯和 T4 血清的變化[1]。
    Bexarotene 是一種有效的預(yù)防肺腫瘤生長和進展的藥物。Bexarotene (100 mg/kg by gavage) 抑制所有三種基因型小鼠的腫瘤多樣性和腫瘤體積 (p53wt/wtK-raswt/wt，p53val135/wtK-raswt/wt，或 p53wt/wtK-rasko/wt) . 在 p53wt/wtK-rasko/wt 和 p53wt/wtK-raswt/wt 小鼠中，Bexarotene 將腺瘤向腺癌的進展降低了約 50%[3]。

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

    Animal Model: UL53-3 mice (p53wt/wtK-raswt/wt, p53val135/wtK-raswt/wt, or p53wt/wtK-rasko/wt)[3]
    Dosage: 100?mg/kg
    Administration: Gavage with 18 gage of gavage-needle, 0.1?mL per mouse per day, 5 times a week, continued for 12 weeks
    Result: Inhibited both tumor multiplicity and tumor volume in mice of all three genotypes.
    Clinical Trial
    分子量

    348.48

    Formula

    C24H28O2
    CAS 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    貝沙羅??；蓓薩羅丁
    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性數(shù)據(jù)
    細胞實驗： 

    DMSO 中的溶解度 : 60 mg/mL (172.18 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.8696 mL 14.3480 mL 28.6961 mL
    5 mM 0.5739 mL 2.8696 mL 5.7392 mL
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

    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

    動物實驗：

    請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，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

      請依序添加每種溶劑： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 2.62 mg/mL (7.52 mM); 懸濁液; 超聲助溶

    • 方案 二

      請依序添加每種溶劑： 5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: 2.62 mg/mL (7.52 mM); 懸濁液; 超聲助溶

    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動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。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，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，請謹慎選擇該方案。
    請確保第一步儲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: 99.92%

    參考文獻

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(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 2.8696 mL 14.3480 mL 28.6961 mL 71.7401 mL
    5 mM 0.5739 mL 2.8696 mL 5.7392 mL 14.3480 mL
    10 mM 0.2870 mL 1.4348 mL 2.8696 mL 7.1740 mL
    15 mM 0.1913 mL 0.9565 mL 1.9131 mL 4.7827 mL
    20 mM 0.1435 mL 0.7174 mL 1.4348 mL 3.5870 mL
    25 mM 0.1148 mL 0.5739 mL 1.1478 mL 2.8696 mL
    30 mM 0.0957 mL 0.4783 mL 0.9565 mL 2.3913 mL
    40 mM 0.0717 mL 0.3587 mL 0.7174 mL 1.7935 mL
    50 mM 0.0574 mL 0.2870 mL 0.5739 mL 1.4348 mL
    60 mM 0.0478 mL 0.2391 mL 0.4783 mL 1.1957 mL
    80 mM 0.0359 mL 0.1794 mL 0.3587 mL 0.8968 mL
    100 mM 0.0287 mL 0.1435 mL 0.2870 mL 0.7174 mL
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    產(chǎn)品名稱：
    Bexarotene
    目錄號：
    HY-14171
    需求量：