GCN2-IN-7|cas:2396465-33-9|西域试剂

GCN2-IN-7,99.58%

产品编号：Bellancom-151460| CAS NO：2396465-33-9| 分子式：C₂₂H₂₃BrN₈OS| 分子量：527.44

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	包装	价格	库存与货期	购买量	操作
Bellancom-151460		￥3800.00	杭州北京（现货）
Bellancom-151460		￥9500.00	杭州北京（现货）

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GCN2-IN-7

产品介绍

GCN2-IN-7 (compound 39) 是一种具有口服活性和选择性的 general control nonderepressible 2 (GCN2) 抑制剂 (IC₅₀=5 nM)，具有体内的抗肿瘤活性。

生物活性

GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC₅₀=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo.

体外研究

GCN2-IN-7 (600 nM; 3 d) alleviates myeloid-derived suppressive cells (MDSC)-related T cell suppression and restores T cell proliferation.

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

Cell Proliferation Assay

Cell Line:	CD8⁺ T cells from WT and GCN2KO cells
Concentration:	600 nM
Incubation Time:	3 days
Result:	Relieved MDSC suppression of proliferation of the co-cultured CD8⁺ T cells with significant relief at 600 nM.

体内研究
(In Vivo)

GCN2-IN-7 (oral gavage; 15 mg/kg; BID; 17 d) shows robust target engagement in vivo at a reasonable dose.
GCN2-IN-7 (oral gavage; 50 mg/kg; BID; 17 d) inhibits tumor growth in vivo of the LL2 syngeneic mouse tumor model.

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

Animal Model:	Balb/c mice injected with RENCA cells
Dosage:	15 mg/kg
Administration:	Oral gavage; 15 mg/kg; BID; 17 days
Result:	Showed robust target engagement of GCN2 in both tumor (average of 84%) and spleen (average of 80%) tissues. Showed an average of 65% reduction of downstream marker Activation Transcription Factor 4 (ATF4) in compound-treated mice compared to the vehicle treatment group.

Animal Model:	LL2 syngeneic mouse model
Dosage:	50 mg/kg
Administration:	Oral gavage; 50 mg/kg; BID; 17 days
Result:	Showed tumor growth inhibition (56%) after 26 days of dosing compared to the vehicle group.

体内研究

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

Animal Model:	Balb/c mice injected with RENCA cells
Dosage:	15 mg/kg
Administration:	Oral gavage; 15 mg/kg; BID; 17 days
Result:	Showed robust target engagement of GCN2 in both tumor (average of 84%) and spleen (average of 80%) tissues. Showed an average of 65% reduction of downstream marker Activation Transcription Factor 4 (ATF4) in compound-treated mice compared to the vehicle treatment group.

Animal Model:	LL2 syngeneic mouse model
Dosage:	50 mg/kg
Administration:	Oral gavage; 50 mg/kg; BID; 17 days
Result:	Showed tumor growth inhibition (56%) after 26 days of dosing compared to the vehicle group.

体内研究

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

Animal Model:	Balb/c mice injected with RENCA cells
Dosage:	15 mg/kg
Administration:	Oral gavage; 15 mg/kg; BID; 17 days
Result:	Showed robust target engagement of GCN2 in both tumor (average of 84%) and spleen (average of 80%) tissues. Showed an average of 65% reduction of downstream marker Activation Transcription Factor 4 (ATF4) in compound-treated mice compared to the vehicle treatment group.

Animal Model:	LL2 syngeneic mouse model
Dosage:	50 mg/kg
Administration:	Oral gavage; 50 mg/kg; BID; 17 days
Result:	Showed tumor growth inhibition (56%) after 26 days of dosing compared to the vehicle group.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (189.60 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8960 mL	9.4798 mL	18.9595 mL
5 mM	0.3792 mL	1.8960 mL	3.7919 mL
10 mM	0.1896 mL	0.9480 mL	1.8960 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 (sealed storage, away from moisture and light)。-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 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.74 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.74 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。