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LAS17

产品编号 T39906 CAS 2362527-67-9

别名: LAS17

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.

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LAS17, CAS 2362527-67-9

规格	价格/CNY	货期
2 mg	￥ 1,370	5日内发货
5 mg	￥ 2,760	5日内发货
1 mL * 10 mM (in DMSO)	￥ 2,790	5日内发货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	LAS17, a potent and selective irreversible inhibitor targeting tyrosine in glutathione S-Transferase Pi (GSTP1), effectively inhibits GSTP1 activity, demonstrated by an IC50 value of 0.5 μM.
体外活性	Glutathione?S-Transferase Pi (GSTP1) mediates cellular defense against reactive electrophiles. LAS17 inhibits GSTP1 activity?in vitro?in a concentration-dependent manner[1]. 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[2]. GSTP1 knockdown in LAS17 (10 μM) treatment in 231MFP cells results in increased levels of phosphorylated AMPK and acetyl CoA carboxylase (ACC)[2]. 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[2]. Cell Viability Assay[2]Cell 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 Analysis[2]Cell Line: 231MFP cells Concentration: 10 μM Incubation Time: Result: LAS17-treated?231MFP cells show increased levels of phosphorylated AMPK and ACC.
体内活性	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[2]. Animal Model: Severe combined immunodeficiency (SCID) mice bearing 231MFP tumor xenograft[2]Dosage: 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.

别名	LAS17
分子量	359.25
分子式	C15H20Cl2N4O2
CAS No.	2362527-67-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. L A Crawford, et al. A tyrosine-reactive irreversible inhibitor for glutathione S-transferase Pi (GSTP1). Mol Biosyst. 2016 May 24;12(6):1768-71. 2. Sharon M Louie, et al. GSTP1 Is a Driver of Triple-Negative Breast Cancer Cell Metabolism and Pathogenicity. Cell Chem Biol. 2016 May 19;23(5):567-578.

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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