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SAR405

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Chemical Structure| 1523406-39-4 同义名 : -
CAS号 : 1523406-39-4
货号 : A195150
分子式 : C19H21ClF3N5O2
纯度 : 98+%
分子量 : 443.851
MDL号 : MFCD28411361
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(56.33 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

2% DMSO+30% PEG 300+2% Tween 80+water 4 mg/mL

生物活性
靶点

  • Vps34

    Vps34, IC50:1.2 nM
描述 SAR405 is a pioneering, selective, ATP-competitive inhibitor of the PI3K class III isoform Vps34 (PIK3C3) (IC50=1.2 nM; KD=1.5 nM). It suppresses autophagy triggered by either starvation or mTOR inhibition and exhibits anticancer properties [1][2].
作用机制 SAR405 has an exquisite protein and lipid kinase selectivity profile due to its unique binding mode and molecular interactions within the ATP binding cleft of human Vps34.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.25mL

0.45mL

0.23mL

11.27mL

2.25mL

1.13mL

22.53mL

4.51mL

2.25mL
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.