GCN2-IN-6|cas:2183470-09-7|西域试剂

GCN2-IN-6,99.03%

产品编号：Bellancom-130240| CAS NO：2183470-09-7| 分子式：C₁₉H₁₂Cl₂F₂N₄O₃S| 分子量：485.29

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-130240	￥3500.00	杭州北京（现货）
Bellancom-130240	￥5500.00	杭州北京（现货）
Bellancom-130240	￥16500.00	杭州北京（现货）
Bellancom-130240	￥28000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

GCN2-IN-6

产品介绍

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)。

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.

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

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.

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

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.

体内研究

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

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.

性状

Solid

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。
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: ≥ 2.08 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。