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SAR405
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SAR405图片
CAS NO:1523406-39-4
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
SAR-405 是一种选择性 PIK3C3/Vps34 抑制剂,IC50为1.2 nM,Kd为1.5 nM,可防止自噬并与肿瘤细胞中的 mTOR 抑制协同作用。它抑制饥饿或 mTOR 抑制诱导的自噬,具有抗癌活性。

产品描述

SAR-405 is a potent and selective PIK3C3/Vps34 inhibitor (IC50:1.2 nM; Kd:1.5 nM) that prevents autophagy and synergizes with MTOR inhibition in tumor cells. SAR405 treatment also inhibits autophagy induced either by starvation or by MTOR (mechanistic target of rapamycin) inhibition. Combining SAR405 with everolimus results in a significant synergy on the reduction of cell proliferation using renal tumor cells.

体外活性

SAR405, a low molecular mass kinase inhibitor of PIK3C3, highly potent and selective with regard to other lipid and protein kinases.?Inhibiting the catalytic activity of PIK3C3 disrupts vesicle trafficking from late endosomes to lysosomes.?SAR405 treatment also inhibits autophagy induced either by starvation or by MTOR (mechanistic target of rapamycin) inhibition.?SAR405 prevents autophagosome formation (IC50: 42 nM).?Treatment of starved cells with SAR405 fully inhibits the conversion to LC3-II in a dose-dependent manner.?The GFP-LC3 model is used for the HTS and confirmed its activity on starved cells (IC50=419 nM) [1][2].

Cas No.

1523406-39-4

分子式

C19H21ClF3N5O2

分子量

443.85

储存和溶解度

DMSO:27 mg/mL (60.83 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years