LAS17
目录号: PL02270 纯度: ≥97%
CAS No. :2362527-67-9
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中文名称
LAS17
英文名称
LAS17
英文别名
LAS17;methyl (2R)-2-[(4,6-dichloro-1,3,5-triazin-2-yl)-pent-4-ynylamino]-4-methylpentanoate
Cas No.
2362527-67-9
分子式
C15H20Cl2N4O2
分子量
359.25
包装储存
Pure form -20°C 3 years;In solvent -80°C 6 months
产品详情
LAS17 是一种强效的,不可逆的,选择性谷胱甘肽 S-转移酶 Pi (GSTP1) 抑制剂。LAS17 抑制 GSTP1 活性,IC50 为 0.5 µM.
生物活性
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.
性状
Oil
体外研究(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. has not independently confirmed the accuracy of these methods.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Pure form -20°C 3 years;In solvent -80°C 6 months
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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (278.36 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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