GCN2-IN-6 - CAS:2183470-09-7

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GCN2-IN-6

目录号 : KM7555 CAS No. : 2183470-09-7 纯度 : 98%

Data Sheet 产品使用指南

GCN2-IN-6 (Compound 6d) 是一种有效的口服 GCN2 抑制剂，通过酶法 (IC₅₀ 为 1.8 nM) 和细胞分析 (IC₅₀ 为 9.3 nM) 证实。GCN2-IN-6 还是 eIF2α 激酶 PERK 抑制剂，IC₅₀ 为 0.26 nM (酶法测定) 和 230 nM (细胞测定)。

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10mg		In-stock
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500mg	询价	In-stock

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生物活性

GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC₅₀ of 1.8 nM) and cellular assays (IC₅₀ of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC₅₀ of 0.26 nM (in enzymatic assay) and 230 nM (in cells).

体外研究

To examine the impact of GCN2 inhibition on cancer cell proliferation, acute lymphoblastic leukemia (ALL) CCRFCEM cells are treated with GCN2-IN-6 (Compound 6d) in the presence of asparaginedepleting agent asparaginase. Treatment with GCN2-IN-6 greatly sensitizes CCRF-CEM cells to asparaginase. The moderate antiproliferative effects achieved by combining asparaginase and GCN2-IN-6 treatment are observed in GCN2-wildtype (WT) mouse embryonic fibroblast (MEF) cells but not in GCN2-knockout (KO) MEF. GCN2-IN-6 demonstrates suppression on p-GCN2, p-eIF2α, and ATF4 activated by asparaginase.

体内研究

GCN2-IN-6 (Compound 6d; 0.3-3 mg/kg; oral administration; for 8 hours; mice) treatment at 3 mg/kg suppresses both self-phosphorylation of GCN2 and the downstream effector ATF4 to the basal level following pretreatment with asparaginase.

Animal Model:	Mice bearing CCRF-CEM cells xenografts
Dosage:	0.3 mg/kg, 1 mg/kg, and 3 mg/kg
Administration:	Oral administration; for 8 hours
Result:	Suppressed both self-phosphorylation of GCN2 and the downstream effector ATF4 to the basal level following pretreatment with asparaginase.

分子式

C₁₉H₁₂Cl₂F₂N₄O₃S

分子量

485.29

CAS号

2183470-09-7

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 : 250 mg/mL (515.16 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0606 mL	10.3031 mL	20.6062 mL
5 mM	0.4121 mL	2.0606 mL	4.1212 mL
10 mM	0.2061 mL	1.0303 mL	2.0606 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: ≥ 2.08 mg/mL (4.29 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.29 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.29 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.29 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。