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SAR405

Catalog No. T12831L   CAS 1523406-39-4

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.

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SAR405 Chemical Structure
SAR405, CAS 1523406-39-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 48.00
2 mg In stock $ 72.00
5 mg In stock $ 105.00
10 mg In stock $ 189.00
25 mg In stock $ 378.00
50 mg In stock $ 579.00
1 mL * 10 mM (in DMSO) In stock $ 98.00
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Purity: 99.79%
Purity: 99.42%
Purity: 99.27%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 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.
Targets&IC50 Autophagy:, VPS34:1.2 nM, VPS34:1.5 nM (kd)
In vitro 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].
Molecular Weight 443.85
Formula C19H21ClF3N5O2
CAS No. 1523406-39-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 27 mg/mL (60.83 mM)

TargetMolReferences and Literature

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.

TargetMolCitations

1. Liu Y, Sun Y, Xu Y, et al.Targeting VPS41 induces methuosis and inhibits autophagy in cancer cells.Cell Chemical Biology.2023

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Inhibitor Library Kinase Inhibitor Library Anti-Ovarian Cancer Compound Library Angiogenesis related Compound Library NO PAINS Compound Library Autophagy Compound Library Anti-Pancreatic Cancer Compound Library Anti-Cancer Metabolism Compound Library Neural Regeneration Compound Library

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Keywords

SAR405 1523406-39-4 Autophagy PI3K/Akt/mTOR signaling PI3K inhibit Inhibitor Phosphoinositide 3-kinase SAR 405 SAR-405 inhibitor

 

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