GNE-049|cas:1936421-41-8|西域试剂

GNE-049,98.00%

产品编号：Bellancom-108435| CAS NO：1936421-41-8| 分子式：C₂₇H₃₂F₂N₆O₂| 分子量：510.58

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-108435	￥5500.00	杭州北京（现货）
Bellancom-108435	￥8500.00	杭州北京（现货）
Bellancom-108435	￥27500.00	杭州北京（现货）
Bellancom-108435	￥39500.00	杭州北京（现货）

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GNE-049

产品介绍

GNE-049 是一种高效的选择性 CBP 抑制剂，在 TR-FRET 实验中 IC₅₀ 为 1.1 nM。GNE-049 还抑制 BRET 和 BRD4(1)，IC₅₀ 分别为 12 nM 和 4200 nM。

生物活性

GNE-049 is a highly potent and selective CBP inhibitor with an IC₅₀ of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC₅₀s of 12 nM and 4200 nM, respectively.

体外研究

GNE-049 is selected for further profiling as it has the best balance of liver microsomes (LM) stability, selectivity, and cellular potency GNE-049 has excellent potency in the BRET cellular assay and, in an orthogonal measure of the target engagement, GNE-049 is shown to inhibit the expression of MYC (MV4-11 cell line) with an EC₅₀ of 14 nM.

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

体内研究

GNE-049 demonstrates acceptable PK in mouse, rat, dog, and monkey. Determination of potency versus a selection of bromodomains revealed that GNE-049 is selective for CBP/P300 and, importantly, quite selective (3820-fold) over BRD4(1). GNE-049 is further evaluated in a rat single dose (30-250 mg/kg QD) toxicokinetic study. Adverse central nervous system (CNS)-related signs (e.g., marked hyperactivity and vocalization) are observed in several of the rats at the 250 mg/kg dose level. Furthermore, at the 250 mg/kg dose level, the ratio of the unbound drug concentration in brain to unbound drug concentration in plasma (K_p,uu) 3 h post dose is determined to be 0.43, indicating that GNE-049 is penetrating into the CNS and potentially resulting in the observed toxicity.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (195.86 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9586 mL	9.7928 mL	19.5856 mL
5 mM	0.3917 mL	1.9586 mL	3.9171 mL
10 mM	0.1959 mL	0.9793 mL	1.9586 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： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.90 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% corn oil
Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.90 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。