LAS17 - CAS:2362527-67-9

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LAS17

目录号 : KM5593 CAS No. : 2362527-67-9 纯度 : 98%

Data Sheet 产品使用指南

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.

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

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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 IC₅₀ of 0.5 µM.

体外研究

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.

Cell Viability Assay

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

Cell Line:	231MFP cells
Concentration:	10 µM
Incubation Time:
Result:	LAS17-treated 231MFP cells show increased levels of phosphorylated AMPK and ACC.

体内研究

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.

Animal Model:	Severe combined immunodeficiency (SCID) mice bearing 231MFP tumor xenograft
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.

分子式

C₁₅H₂₀Cl₂N₄O₂

分子量

359.25

CAS号

2362527-67-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度： 98%

Data Sheet

产品使用指南

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Other Forms of Rapamycin:

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