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  3. GSK1324726A

GSK1324726A  (Synonyms: I-BET726)

目录号: HY-13960 纯度: 98.49%
COA 产品使用指南

GSK1324726A 是一种有效的选择性 BET 蛋白抑制剂,高亲和力结合到 BRD2 (IC50=41 nM),BRD3 (IC50=31 nM) 和 BRD4 (IC50=22 nM)。

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GSK1324726A Chemical Structure

GSK1324726A Chemical Structure

CAS No. : 1300031-52-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥990
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5 mg ¥900
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10 mg ¥1450
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25 mg ¥2900
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50 mg ¥4300
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100 mg ¥6450
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Top Publications Citing Use of Products

    GSK1324726A purchased from MCE. Usage Cited in: J Med Chem. 2018 Jan 25;61(2):504-513.  [Abstract]

    Protein degradation profile of VHL-based BET degraders. Sub-confluent HeLa cells are treated for 24 h with varying concentration of test compounds JQ1(Compound 3), I-BET726 (Compound 4). Protein extracts are separated by SDS-PAGE and then analyzed by Western blot. Proteins Brd4, Brd3, Brd2 and β-actin are probed for JQ1and I-BET726 with specific antibodies.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    GSK1324726A is a novel, potent, and selective inhibitor of BET proteins with high affinity to BRD2 (IC50=41 nM), BRD3 (IC50=31 nM), and BRD4 (IC50=22 nM).

    IC50 & Target

    IC50: 22 nM (BRD4), 31 nM (BRD3), 41 nM (BRD2)[1]

    体外研究
    (In Vitro)

    A panel of neuroblastoma cell lines are treated with GSK1324726A (I-BET726), and observed potent growth inhibition and cytotoxicity in most cell lines irrespective of MYCN copy number or expression level. All neuroblastoma cell lines tested exhibit potent growth inhibition, with a median growth IC50 value (gIC50; inhibitor concentration resulting in 50% growth inhibition) equal to 75 nM[1].

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

    体内研究
    (In Vivo)

    GSK1324726A (I-BET726) inhibits neuroblastoma tumor growth. In the SK-N-AS model, mice in the vehicle group are euthanized on day 14 due to large tumor size. While there is no significant difference in tumor growth between the vehicle and GSK1324726A (5 mg/kg) group, 58% tumor growth inhibition (TGI) is observed in the GSK1324726A (15 mg/kg) group on day 14 of the study (n=9; p=0.006). Mice in the GSK1324726A (15 mg/kg) group are treated for an additional 7 days before tumor volume reaches a level comparable to that observed in the vehicle group, at which point the study is terminated. Tumors in the CHP-212 model grow much more slowly. After 42 days, tumors in vehicle-treated mice are only half the size those in the SK-N-AS model at the end of the study (Day 14). In the CHP-212 model, treatment with 5 mg/kg GSK1324726A results in TGI equal to 50% (n=8; p=0.1816), and mice in the 15 mg/kg group exhibits a TGI of 82% at the end of the study (n=5; p=0.0488)[1].

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

    分子量

    434.91

    Formula

    C25H23ClN2O3

    CAS 号
    性状

    固体

    颜色

    White to light yellow

    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 : ≥ 46 mg/mL (105.77 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 2.2993 mL 11.4966 mL 22.9933 mL
    5 mM 0.4599 mL 2.2993 mL 4.5987 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: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.75 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。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.75 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,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    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: 98.49%

    参考文献
    Cell Assay
    [1]

    Cell line growth-death assays are performed with a few modifications. Briefly, cells are seeded into 384-well or 96-well plates at a density optimized for 6 days of growth. The following day, T0 measurements are taken using CellTiter-Glo, CellTiter-Fluor, or CyQuant Direct. Plates are read on an Envision, Safire 2, or SpectraMax Gemini EM plate reader. Remaining plates are treated with DMSO or a titration of GSK1324726A. Cells are incubated for 6 days and developed. Results are plotted as a percentage of the T0 value, normalized to 100%, versus concentration of compound. A 4-parameter equation is used to generate concentration response curves. Growth IC50 (gIC50) values are calculated at the mid-point of the growth window (between DMSO and T0 values). Ymin-T0 values are calculated by subtracting the T0 value (100%) from the Ymin value on the curve, and are a measure of net population cell growth or death[1].

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

    Animal Administration
    [1][2]

    Mice[1]
    CHP-212 (1×107) or SK-N-AS (5×106) cells in 100% matrigel are implanted subcutaneously into the right flank of approximately 9 week old female nude (Crl:CD-1-Foxn1 nu) mice. Tumors are measured with calipers and randomized using stratified sampling according to tumor size into treatment groups of 10 mice. GSK1324726A in vehicle or vehicle alone is administered orally by individual body weight at 10mls/kg. Mice are weighed and tumors are measured with calipers twice weekly, and mice are observed daily for any adverse treatment affects. Mice are euthanized using CO2 inhalation according to AVMA guidelines after two consecutive tumor measurements greater than 2500mm3, or if body weight loss greater than 20% is observed. For mouse pharmacodynamic studies, mice are euthanized as described above. Tumors are harvested from euthanized mice and placed in RNAlater for RNA isolation. Blood is collected after euthanasia via cardiac puncture.
    Rats[2]
    Male CD rats (253-283 g) are surgically prepared with implanted cannulae in the femoral vein (for GSK1324726A administration) and jugular vein (for blood sampling). Each rat receives Duphacillin (100 mg/kg s.c.) and Carprofen (7.5 mg/kg s.c.) as a pre-operative antibiotic and analgesic respectively. Each rat is allowed to recover for at least 2 days prior to dosing. Rats have free access to food and water throughout. Rat PK studies are conducted as a crossover design over 2 dosing occasions, with 3 days between dose administrations. Serial blood samples are taken (via indwelling jugular cannula) up to 26 h post dose administration on both dosing occasions. On study day 1, n=3 male rats each receives a 1 h intravenous infusion of GSK1324726A formulated in DMSO and 10% (w/v) KleptoseTM in saline (2%:98%) at a concentration of 0.2 mg/mL and the dose is filtered using a ca. 0.2 μm syringe filter unit. GSK1324726A is administered as a 1 h i.v. infusion at 5 mL/kg/h to achieve a target dose of 1 mg/kg. On study day 2, the same three rats each receives an oral administration of GSK1324726A suspended in 3% Pharmacoat 603/0.2% Sodium Lauryl Sulphate (w/v) aq. at a concentration of 0.6 mg/mL administered by gavage at 5 mL/kg to achieve a target dose of 3 mg/kg. At the end of the study the rats are euthanised by administration of sodium pentobarbital through the jugular vein cannula.

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

    参考文献

    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 2.2993 mL 11.4966 mL 22.9933 mL 57.4832 mL
    5 mM 0.4599 mL 2.2993 mL 4.5987 mL 11.4966 mL
    10 mM 0.2299 mL 1.1497 mL 2.2993 mL 5.7483 mL
    15 mM 0.1533 mL 0.7664 mL 1.5329 mL 3.8322 mL
    20 mM 0.1150 mL 0.5748 mL 1.1497 mL 2.8742 mL
    25 mM 0.0920 mL 0.4599 mL 0.9197 mL 2.2993 mL
    30 mM 0.0766 mL 0.3832 mL 0.7664 mL 1.9161 mL
    40 mM 0.0575 mL 0.2874 mL 0.5748 mL 1.4371 mL
    50 mM 0.0460 mL 0.2299 mL 0.4599 mL 1.1497 mL
    60 mM 0.0383 mL 0.1916 mL 0.3832 mL 0.9581 mL
    80 mM 0.0287 mL 0.1437 mL 0.2874 mL 0.7185 mL
    100 mM 0.0230 mL 0.1150 mL 0.2299 mL 0.5748 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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    产品名称:
    GSK1324726A
    目录号:
    HY-13960
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