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SAR405

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。

CAS号

1523406-39-4

分子式

C19H21ClF3N5O2

主要靶点

Autophagy|PI3K

仅限科研使用

Cat No : CM05966

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Synonyms

验证数据展示

  • CAS No.: 1523406-39-4

    SAR405
    CAS#: 1523406-39-4

产品信息

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.

CAS号 1523406-39-4
分子式 C19H21ClF3N5O2
主要靶点 Autophagy|PI3K
主要通路 自噬|PI3K/Akt/mTOR信号通路
分子量 443.85
纯度 99.42%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

Vps34:1.2 nM|Vps34:1.5 nM (kd)|Autophagy:

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].

溶解度

DMSO:27 mg/mL (60.83 mM)

参考文献

1.Ronan B, et al. A highly potent and selective Vps34 inhibitor alters vesicle trafficking and autophagy. Nat Chem Biol. 2014 Dec;10(12):1013-9.
2.Pasquier B. SAR405, a PIK3C3/Vps34 inhibitor that prevents autophagy and synergizes with MTOR inhibition in tumor cells. Autophagy. 2015 Apr 3;11(4):725-6.

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