LAS17

CAS: 2362527-67-9 货号: L654922 分子式: C15H20Cl2N4O2 分子量: 359.25 PubChem CID: 156024492
有货
级别和纯度: 10mM in DMSO
储存条件
-80℃储存
运输条件
特低温运输
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规格
库存
价格
数量
1ml
L654922-1ml
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¥3,080.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


LAS17 is a potent and selective tyrosine-directed irreversible inhibitor for glutathione S-Transferase Pi ( GSTP1 ). LAS17 inhibits GSTP1 activity with an IC 50 of 0.5 µM .

In Vitro

Glutathione S-Transferase Pi (GSTP1) mediates cellular defense against reactive electrophiles. LAS17 inhibits GSTP1 activity in vitro in a concentration-dependent manner. LAS17 (10 µM; Serum-free survival 48 h) treatment in 231MFP breast cancer cells recapitulates the serum-free cell survival impairments observed with genetic inactivation of GSTP1. GSTP1 knockdown in LAS17 (10 µM) treatment in 231MFP cells results in increased levels of phosphorylated AMPK and acetyl CoA carboxylase (ACC). LAS17 treatment in 231MFP cells also shows reduced levels of ATP, lactic acid, purine nucleotides, and diacylated phospholipids and alkylacyl ether lipids and increased levels of acyl carnitines (ACs), ceramides, lysophospholipids. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: 231MFP breast cancer cells Concentration: 10 µM Incubation Time: 48 hours Result: Recapitulated the serum-free cell survival impairments observed with genetic inactivation of GSTP1. Western Blot AnalysisCell Line: 231MFP cells Concentration: 10 µM Incubation Time: Result: LAS17-treated 231MFP cells show increased levels of phosphorylated AMPK and ACC.

In Vivo

Daily administration of LAS17 (20 mg/kg ip, once per day) significantly impairs 231MFP breast tumor xenograft growth in immune-deficient mice when treatment is initiated 2 days after subcutaneous injection of cells, and LAS17 even slows tumor growth when initiated 16 days after tumor implantation, with no observable toxicity and no weight-change. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Severe combined immunodeficiency (SCID) mice bearing 231MFP tumor xenograftDosage: 20 mg/kg (prepared in PBS:ethanol:PEG40 (18:1:1)) Administration: Daily administration i.p., once per day Result: Significantly impaired 231MFP breast tumor xenograft growth.

规格

规格或纯度
10mM in DMSO
英文名称
LAS17
生化机理
LAS17 是一种强效、选择性的酪氨酸定向不可逆谷胱甘肽转移酶 Pi(GSTP1)抑制剂。LAS17 抑制 GSTP1 活性的 IC 50 为 0.5 µM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
PubChem CID
分子量
359.25

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