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  3. Birabresib

Birabresib  (Synonyms: OTX-015; MK-8628)

目录号: HY-15743 纯度: 99.87%
COA 产品使用指南

Birabresib (OTX-015) 是一种有效的 BRD2/3/4 抑制剂,IC50 值为 92-112 nM。

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Birabresib Chemical Structure

Birabresib Chemical Structure

CAS No. : 202590-98-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1072
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2 mg ¥500
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5 mg ¥990
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10 mg ¥1500
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50 mg ¥4100
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100 mg ¥7000
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500 mg   询价  

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Customer Review

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Top Publications Citing Use of Products

    Birabresib purchased from MCE. Usage Cited in: Cancer Res. 2019 May 15;79(10):2761-2774.  [Abstract]

    Western blot analysis of HER3 in SCCOHT1 cells after re-expression and dose-dependent treatment with OTX015 at 24h.

    Birabresib purchased from MCE. Usage Cited in: Cancer Res. 2019 May 15;79(10):2761-2774.  [Abstract]

    BETi dampens signaling downstream of receptor tyrosine kinases. Western blotting of HER3 and downstream effectors in response to increasing doses of OTX015 at 24h. SCCOHT1, OVK18: SCCOHT cells; OVCAR8, SKOV3, and IGROV1, serous ovarian carcinoma cells.

    Birabresib purchased from MCE. Usage Cited in: EMBO Mol Med. 2018 May;10(5). pii: e8446.  [Abstract]

    NRAS-mutant melanoma cells grown as collagen-embedded 3D spheroids are treated with DMSO, 0.1 μM MEKi PD901, 0.5 μM BETi (JQ-1 or OTX-015), or BETi+MEKi combination for 5 days. Spheroids are stained with Calcein (AM) (green; live cells) and EtBr (red; dead cells) and imaged using a fluorescence microscope.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC50s ranging from 92 to 112 nM.

    IC50 & Target

    IC50: 92-112 nM (BRD2, BRD3, BRD4)[1]

    体外研究
    (In Vitro)

    Birabresib (OTX-015) (500 nM) exposure induces a strong decrease of BRD2, BRD4 and c-MYC and increase of HEXIM1 proteins, while BRD3 expression is unchanged. c-MYC, BRD2, BRD3, BRD4?and?HEXIM1?mRNA levels do correlate however with viability following exposure to Birabresib (OTX-015)[2].?Birabresib (OTX-015) (0.1, 1, 5 μM) treatment induces HIV-1 full-length transcripts and viral outgrowth in resting CD4+ T cells from infected individuals receiving suppressive antiretroviral therapy (ART), while exerting minimal toxicity and effects on T cell activation. Birabresib-mediated activation of HIV-1 involves an increase in CDK9 occupancy and RNAP II C-terminal domain (CTD) phosphorylation[3].

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

    体内研究
    (In Vivo)

    In MDA-MB-231 murine xenografts, tumor mass is significantly (p?< 0.05) reduced by Birabresib (OTX-015) (50 mg/kg) with respect to vehicle-treated animals. Birabresib (OTX-015) in combination with 2 mg/kg RAD001 shows more effective activity than Birabresib alone[4].

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

    Clinical Trial
    分子量

    491.99

    Formula

    C25H22ClN5O2S

    CAS 号
    性状

    固体

    颜色

    Off-white to gray

    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
    In Vitro: 

    DMSO 中的溶解度 : ≥ 49 mg/mL (99.60 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.0326 mL 10.1628 mL 20.3256 mL
    5 mM 0.4065 mL 2.0326 mL 4.0651 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)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    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

    • 方案 一

      请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 3 mg/mL (6.10 mM); 澄清溶液

    • 方案 二

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

      Solubility: ≥ 2.5 mg/mL (5.08 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。

      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。

    以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 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: 50% PEG300    50% Saline

      Solubility: 10 mg/mL (20.33 mM); 澄清溶液; 超声助溶 (<60°C)

    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

    g

    每只动物的给药体积

    μL

    动物数量

    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: 99.87%

    参考文献
    Cell Assay
    [2]

    For the MTT assay, cells are seeded in 24-well plates at 1×106 per well and treated with Birabresib (OTX-015) (0.01 nM-10 μM) for 72 h. Cells are transferred to 96-well plates and incubated with 0.5 mg/mL 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) in the dark at 37°C for 4 h. Cells are then lysed with 25% sodium dodecyl sulfate (SDS) lysis buffer and absorbance is read at 570 nm using a Microplate Reader. Three independent experiments are run for each cell line and untreated cells are used as negative controls.

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

    Animal Administration
    [4]

    Mice are subcutaneously injected in the right flank with 10×106 MDA-MB-231 cells. When average tumor weight is appr 130 mg, mice are randomized (nine animals/group) to one of the following experimental groups: vehicle (for Birabresib (OTX-015), water, twice daily, oral; for RAD001 vehicle, 5% Tween-80/5% polyethylene glycol 400, thrice weekly, intraperitoneal); 50 mg/kg Birabresib (OTX-015), twice daily, oral; 2 mg/kg RAD001, thrice weekly, intraperitoneal; 50 mg/kg Birabresib (OTX-015) + 2 mg/kg RAD001, according to the single agent dosing schedules.

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

    参考文献

    Birabresib 相关分类

    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。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0326 mL 10.1628 mL 20.3256 mL 50.8140 mL
    5 mM 0.4065 mL 2.0326 mL 4.0651 mL 10.1628 mL
    10 mM 0.2033 mL 1.0163 mL 2.0326 mL 5.0814 mL
    15 mM 0.1355 mL 0.6775 mL 1.3550 mL 3.3876 mL
    20 mM 0.1016 mL 0.5081 mL 1.0163 mL 2.5407 mL
    25 mM 0.0813 mL 0.4065 mL 0.8130 mL 2.0326 mL
    30 mM 0.0678 mL 0.3388 mL 0.6775 mL 1.6938 mL
    40 mM 0.0508 mL 0.2541 mL 0.5081 mL 1.2704 mL
    50 mM 0.0407 mL 0.2033 mL 0.4065 mL 1.0163 mL
    60 mM 0.0339 mL 0.1694 mL 0.3388 mL 0.8469 mL
    80 mM 0.0254 mL 0.1270 mL 0.2541 mL 0.6352 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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    目录号:
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