1. Epigenetics
  2. Epigenetic Reader Domain
    Histone Acetyltransferase
  3. GNE-781

GNE-781 

目录号: HY-108696 纯度: 98.21%
产品使用指南

GNE-781 是一种有效的,具有口服活性的选择性 CBP 抑制剂,在 TR-FRET 实验中 IC50 为 0.94 nM。GNE-781 还抑制 BRETBRD4 (1)IC50 分别为 6.2 nM 和 5100 nM。GNE-781 在 MOLM-16 AML 异种移植模型中显示抗肿瘤活性。

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GNE-781 Chemical Structure

GNE-781 Chemical Structure

CAS No. : 1936422-33-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3700
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5 mg ¥3200
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10 mg ¥5200
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50 mg ¥15200
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100 mg ¥24300
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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

GNE-781 is an orally active, highly potent and selective CBP inhibitor with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nM, respectively. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model[1].

IC50 & Target

IC50: 0.94 nM (CBP), 6.2 nM (BRET), 5100 nM (BRD4(1))[1]

体外研究
(In Vitro)

GNE-781 is a highly advanced potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein, binding protein (CBP). GNE-781 reduces FOXP3 (forkhead box P3) transcript levels. Examination of a subset of bromodomains reveals that GNE-781 is exquisitely selective for CBP/P300 and is remarkably selective for CBP (5425-fold) and P300 (4250-fold). GNE-781 demonstrates an appropriate balance of cell potency, selectivity (5425-fold over BRD4(1)) [1].

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

体内研究
(In Vivo)

GNE-781 (3-30 mg/kg; p.o.; twice daily for 21 days) has tumor growth inhibition (%TGI) is 73%, 71%, and 89% at 3, 10, and 30 mg/kg, respectively in SCID beige mice with MOLM-16 AML xenografts[1].
GNE-781 decreases Foxp3 transcript levels in a dose dependent manner. GNE-781 (3-30 mg/kg) suppresses MYC at doses as low as 3 mg/kg at 2 and 8 h, with maximal suppression at 10 and 30 mg/kg at 2 h (87% and 88% inhibition, respectively)[1].

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

分子量

525.59

Formula

C27H33F2N7O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

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

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (190.26 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9026 mL 9.5131 mL 19.0262 mL
5 mM 0.3805 mL 1.9026 mL 3.8052 mL
10 mM 0.1903 mL 0.9513 mL 1.9026 mL
*

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 (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。

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

  • 1.

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

    Solubility: ≥ 2.87 mg/mL (5.46 mM); Clear solution

  • 2.

    请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: 2.87 mg/mL (5.46 mM); Suspended solution; Need ultrasonic

  • 3.

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

    Solubility: ≥ 1.67 mg/mL (3.18 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (3.18 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 4.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.67 mg/mL (3.18 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (3.18 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 5.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 1.67 mg/mL (3.18 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (3.18 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
Animal Administration
[1]

Mice[1]
Twelve female CD-1 mice are used. All animals are 6-9 weeks old at the time of study and weighed between 20 and 35 g. Animals (n=3 per dosing route) are dosed with 10 or GNE-781 at 1 mg/kg iv (in propyl ethylene glycol 400 (35% v/v) and water (65% v/v)) or 5 mg/kg po (suspended in 0.5% w/v methylcellulose, 0.2% w/v Tween 80). Food and water are available ad libitum to all animals. Serial blood samples (15 μL) are collected by tail nick at 0.033, 0.083, 0.25, 0.5, 1, 3, 8, and 24 h after the intravenous administration and 0.083, 0.25, 0.5, 1, 3, 8, and 24 h after the oral administration. All blood samples are diluted with 60 μL of water containing 1.7 mg/mL EDTA and kept at -80 °C until analysis[1].
Rats[1]
Twelve male Sprague-Dawley rats are used. All animals are 6-9 weeks old at the time of study and weighed between 200 and 300 g. Animals (n=3 per dosing route) are dosed with 10 or GNE-781 at 1 mg/kg iv (in propyl ethylene glycol 400 (35% v/v) and water (65% v/v)) or 5 mg/kg po (suspended in 0.5% w/v methylcellulose, 0.2% w/v Tween 80). Food and water are available ad libitum to animals in the iv groups. Animals in po groups are fasted overnight and food withheld until 4 h postdose. Approximately 250 μL of blood are collected via the catheter at 0.033, 0.083, 0.25, 0.5, 1, 2, 4, 8, and 24 h after the intravenous or oral administration. All blood samples are collected into tubes containing 5 μL of 0.5 M K2EDTA and processed for plasma. Samples are centrifuged (2500g for 15 min at 4°C) within 1 h of collection, and plasma samples are kept at -80 °C until analysis[1].

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

参考文献

纯度: 98.21%

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产品名称:
GNE-781
目录号:
HY-108696
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