2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. AZD9496 maleate

AZD9496 maleate 是有效,选择性的雌激素受体 (ERα) 拮抗剂，IC50 为 0.28 nM。AZD9496 maleate 是一种口服有效的选择性雌激素受体降解剂 (SERD)。

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AZD9496 maleate Chemical Structure

AZD9496 maleate Chemical Structure

CAS No. : 1639042-28-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1597
In-stock
5 mg ￥1300
In-stock
10 mg ￥2300
In-stock
50 mg ￥7800
In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Other Forms of AZD9496 maleate:

AZD9496 maleate 相关抗体

Top Publications Citing Use of Products

    AZD9496 maleate purchased from MCE. Usage Cited in: J Nutr Biochem. 2020 Sep;83:108438.  [Abstract]

    AZD9496 suppresses NLRP3 inflammasome activation and assembly in DSS-treated C57BL/6 mice.Colon tissue is immunofluorescently stained with Cy5-NLRP3 antibody, PE-ASC antibody, and FITC-Pro-Caspase-1 antibody.

    AZD9496 maleate purchased from MCE. Usage Cited in: J Nutr Biochem. 2020 Sep;83:108438.  [Abstract]

    AZD9496 suppresses NLRP3 inflammasome activation and assembly in vitro. Protein levels of NLRP3, ASC, Caspase-1, and ERα in colon tissues.

    AZD9496 maleate purchased from MCE. Usage Cited in: Cell Prolif. 2019 Jul;52(4):e12612.  [Abstract]

    The expression levels of ERα, DNMT1, ISL1, Ras, Raf1, p‐ERK and ERK are detected by Western blot in MCF-7-OCT4 cells that are treated with AZD9496 (300 nM for 1 h).

    查看 Estrogen Receptor/ERR 亚型特异性产品:

    查看所有亚型
    Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD).

    IC50 & Target

    IC50: 0.28 nM (ERα antagonism), 0.14 nM (ERα downregulation), 0.82 nM (ERα binding)[1]
    体外研究
    (In Vitro)

    The potency of AZD9496 with IC50 of 0.82 nM, 0.14 nM, and 0.28 nM in ERα binding, downregulation, and antagonism, respectively. AZD9496 significantly inhibits MCF-7 cell growth with EC50 of 0.04 nM[1]. Selectivity of AZD9496 over other tested nuclear hormone receptors is high: androgen receptor (AR), IC50=30 μM; glucocorticoid receptor (GR), IC50=9.2 μM; progesterone receptor (PR), IC50=0.54 μM[2].

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

    AZD9496 maleate 相关抗体:
    体内研究
    (In Vivo)

    Significant tumor growth inhibition is observed as low as 0.5 mg/kg dose in the estrogen-dependent MCF-7 xenograft model, where this effect is accompanied by a dose-dependent decrease in PR protein levels, demonstrating potent antagonist activity. Combining AZD9496 with PI3K pathway and CDK4/6 inhibitors lead to further growth-inhibitory effects compared with monotherapy alone. AZD9496, given once daily orally at 5 and 25 mg/kg produced statistically significant increases in uterine weight compared with the ICI 182780 control (P<0.001) but significantly lower than ICI 47699 (P=0.001)[1]. AZD9496 is also tested in a long-term estrogen deprived model (LTED), using the HCC-1428 LTED cell line that grows in the absence of estrogen and is thought to best represent a model of aromatase inhibition. AZD9496 shows significant activity, with a dose of 5 mg/kg giving tumor regressions in this model[2].

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

    558.55

    Formula

    C29H29F3N2O6
    CAS 号
    性状

    固体

    颜色

    Light yellow to brown

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, protect from light, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 100 mg/mL (179.04 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 1.7903 mL 8.9517 mL 17.9035 mL
    5 mM 0.3581 mL 1.7904 mL 3.5807 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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    • 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： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.75 mg/mL (4.92 mM); 澄清溶液

      此方案可获得 ≥ 2.75 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 27.5 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。
    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

    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）。

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    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
    参考文献
    Cell Assay
    [1]

    Effect of AZD9496, ICI 182780, and ICI 47699 on ERα peptide turnover in MCF-7 cells. Cells are grown in steroid-free conditions in SILAC media containing 13C615N4 L-arginine to label ERα peptide as “heavy” (blue line) and then switched to grow in media containing unlabeled L-arginine to label newly synthesized protein as “normal” (red line) with 0.1% DMSO, 300 nM Tamoxife, 100 nM AZD9496, or 100 nM ICI 182780 for the time indicated. Data shown is representative of two independent experiments[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    In vivo efficacy of AZD9496 in MCF-7 xenograft model. MCF-7 xenografts, grown in male SCID mice, are dosed daily with either PEG/captisol (vehicle) or AZD9496 (0.02, 0.1, 0.5, 10, and 50 mg/kg, p.o., q.d.). Tumor growth is measured by caliper at regular intervals and mean tumor volumes plotted for each dosed group.

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

    AZD9496 maleate 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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7904 mL 8.9518 mL 17.9035 mL 44.7588 mL
    5 mM 0.3581 mL 1.7904 mL 3.5807 mL 8.9518 mL
    10 mM 0.1790 mL 0.8952 mL 1.7904 mL 4.4759 mL
    15 mM 0.1194 mL 0.5968 mL 1.1936 mL 2.9839 mL
    20 mM 0.0895 mL 0.4476 mL 0.8952 mL 2.2379 mL
    25 mM 0.0716 mL 0.3581 mL 0.7161 mL 1.7904 mL
    30 mM 0.0597 mL 0.2984 mL 0.5968 mL 1.4920 mL
    40 mM 0.0448 mL 0.2238 mL 0.4476 mL 1.1190 mL
    50 mM 0.0358 mL 0.1790 mL 0.3581 mL 0.8952 mL
    60 mM 0.0298 mL 0.1492 mL 0.2984 mL 0.7460 mL
    80 mM 0.0224 mL 0.1119 mL 0.2238 mL 0.5595 mL
    100 mM 0.0179 mL 0.0895 mL 0.1790 mL 0.4476 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:

    AZD94961639042-28-6AZD 9496AZD-9496Estrogen Receptor/ERRInhibitorinhibitorinhibit

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