1. Epigenetics
  2. Epigenetic Reader Domain
    Histone Acetyltransferase
  3. GNE-272

GNE-272 

目录号: HY-100726 纯度: 99.74%
产品使用指南

GNE-272 是有效和选择性的 CBP/EP300 抑制剂,对 CBP,EP300 和 BRD4 的 IC50 值分别为0.02,0.03 和 13 μM。GNE-272 也是 CBP/EP300 选择性的体内探针。

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GNE-272 Chemical Structure

GNE-272 Chemical Structure

CAS No. : 1936428-93-1

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1774
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2 mg ¥1100
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5 mg ¥1900
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10 mg ¥3000
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50 mg ¥12000
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100 mg ¥19000
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500 mg   询价  

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  • 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-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300[1].

IC50 & Target

IC50: 0.02 μM (CBP), 0.03 μM (EP300), 13 μM (BRD4)[1]

体外研究
(In Vitro)

GNE-272 is exquisitely selective for CBP/ EP300 and remarkably selective (650-fold) over BRD4. When tested at 10 μM in 35 kinase panel and 42 receptors off-target screening panel, GNE-272 does not inhibit any target at >30%. In addition, GNE-272 does not inhibit (>10 μM, top concentration) several cytochrome P450s (3A4, 1A2, 2C9, 2C19, 2D6). The compound has good potency in the BRET cellular assay. In an orthogonal measure of the target engagement, GNE-272 is shown to inhibit the expression of MYC10 (MV4−11 cell line) with an EC50 of 0.91 μM and good correlation between the BRET and MYC cellular assays is observed[1].

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

体内研究
(In Vivo)

GNE-272 demonstrates low clearance following a 1 mg/ kg intravenous dose in a mouse PK experiment and good oral bioavailability when dosed at 100 mg/kg, reaching an unbound Cmax of 26 μM. GNE-272 shows a marked antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model[1].

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

分子量

424.47

Formula

C22H25FN6O2

CAS 号
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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (235.59 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3559 mL 11.7794 mL 23.5588 mL
5 mM 0.4712 mL 2.3559 mL 4.7118 mL
10 mM 0.2356 mL 1.1779 mL 2.3559 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。-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: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.89 mM,饱和度未知) 的澄清溶液。

    以 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;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
  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.89 mM,饱和度未知) 的澄清溶液。

    以 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 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
  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.89 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 25.0 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
Cell Assay
[1]

Human cancer cell lines (MOLM-16, HL-60, LP-1, KMS-34, Pfeiffer, DOHH-2) are treated for 4 h with 5 μM GNE-272 or DMSO control. After 6 days, cell viability is measured by CellTiter-Glo[1].

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

Animal Administration
[1]

Mice: Mice are given 0 (vehicle, 0.5% methylcellulose; 0.2% Tween-80), 12.5, 25, and 50 mg/kg of GNE-272 by gavage, twice daily (BID) for 21 days in a volume of 100 μL. Tumor volumes are measured in two dimensions (length and width) using Ultra CalIV calipers and analyzed using Excel, version 11.2[1].

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

参考文献
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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
GNE-272
目录号:
HY-100726
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