GLS1 Inhibitor - CAS:1832646-52-2

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GLS1 Inhibitor

目录号 : KCM12134 CAS No. : 1832646-52-2 纯度 : ≥98%

Data Sheet 产品使用指南

GLS1 inhibitor is an inhibitor of glutaminase 1 (GLS1; IC = 0.021 μM). It inhibits the growth of NCI H1703 non-small cell lung cancer (NSCLC) cells in vitro (GI = 0.011 μM). GLS1 inhibitor (100 mg/kg) reduces tumor growth, increases tumor levels of glutamine, and decreases tumor levels of glutamate and aspartate in an NCI H1703 mouse xenograft model.

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock

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生物活性

GLS1 Inhibitor is an orally active, allosteric, selective GLS1 inhibitor with an IC₅₀ of 0.021 µM for GLS1 and an IC₅₀ of 0.051 µM for the GLS1 GAC splice variant. GLS1 Inhibitor increases glutamine and decreases glutamate and aspartate. GLS1 Inhibitor exhibits anticancer activity against non-small cell lung cancer. GLS1 Inhibitor can be used for research on non-small cell lung cancer.

IC₅₀&Target

IC₅₀: 0.021 μM (GLS1)

体外研究

GLS1 Inhibitor inhibits the proliferation of NCI-H1703 cells, with a GI₅₀ of 0.011 μM.
GLS1 Inhibitor inhibits the splicing variants of GLS1 and GLS1 GAC, with IC₅₀ values of 0.021 μM and 0.051 μM, respectively.
GLS1 Inhibitor has a hERG IC₅₀>33.3 μM in Chinese hamster ovary cells.

体内研究

GLS1 Inhibitor (100 mg/kg; oral; Once a day; 21 days) was effective in the NCI-H1703 SCID mouse xenograft model, producing 37% tumor growth inhibition by day 21 and reaching a maximum of 73% by day 12, accompanied by changes in tumor glutamine, glutamate, and aspartate biomarkers.

Animal Model:	SCID (male; Charles River Laboratories; NCI-H1703 subcutaneous xenograft)
Dosage:	100 mg/kg
Administration:	p.o. (oral gavage); once daily; 21 days
Result:	Inhibited tumor growth by 37% by day 21. Achieved maximum tumor growth inhibition of 73% on day 12. Doubled tumor glutamine levels relative to control at 4 h and 24 h on day 21. Reduced tumor glutamate and aspartate levels relative to control on day 21. Achieved mean concentration of 3.57 μM at 4 h and 3.63 μM at 24 h after oral dosing. Achieved mean free concentration of 0.582 μM at 4 h and 0.592 μM at 24 h, corresponding to 53-fold and 54-fold free cover over cell GI50.

分子式

C₁₉H₂₁N₇O₂S

分子量

411.48

CAS号

1832646-52-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO: 20 mg/mL (48.61 mM; Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4303 mL	12.1513 mL	24.3025 mL
5 mM	0.4861 mL	2.4303 mL	4.8605 mL
10 mM	0.2430 mL	1.2151 mL	2.4303 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)。-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。

纯度： ≥98%

Data Sheet

产品使用指南

暂无相关参考文献

The molarity calculator equation

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

质量

浓度

体积

分子量*

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

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动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

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动物数量

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第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

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计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器