Home PI3K/Akt/mTOR PI3K inhibitor - Autophagy inhibitor SAR405 For research use only.

SAR405

SAR405 is a low-molecular-mass kinase inhibitor of PIK3C3/Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR. SAR405 prevents autophagy and synergizes with MTOR (mechanistic target of rapamycin) inhibition in tumor cells.

SAR405 Chemical Structure

SAR405 Chemical Structure

CAS No. 1523406-39-4

Purity & Quality Control

SAR405 Related Products

Signaling Pathway

PI3K Signaling Pathways

PI3K Signaling Pathway

Biological Activity

Description SAR405 is a low-molecular-mass kinase inhibitor of PIK3C3/Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR. SAR405 prevents autophagy and synergizes with MTOR (mechanistic target of rapamycin) inhibition in tumor cells.
Targets
Vps34 [1]
1.2 nM
In vitro
In vitro

SAR405 is an inhibitor that was highly specific for Vps34 with regard to protein kinases and other phosphoinositide kinases. SAR405 has an IC50 of 1 nM in the phosphorylation of a PtdIns substrate by human recombinant Vps34 enzyme. This compound shows a binding equilibrium constant KD of 1.52 ± 0.77 nM (± s.d.) and a dissociation rate constant, koff, of 3.03 ± 0.55 10−3/s, corresponding to a residence half-life, t1/2, of 3.8 min. SAR405 does not affect the Akt phosphorylation at concentrations up to 10 μM in the PC3 cell line. SAR405 affects vesicle trafficking from late endosomes to lysosomes. It is also a potent autophagy inhibitor[1].
Cell Research Cell lines GFP-LC3 HeLa cells
Concentrations 1 μM
Incubation Time 4 h
Method

GFP-LC3 HeLa cells are starved for 2 h in EBSS plus 10 μM Vps34 compound or DMSO. For mTOR inhibitor, GFP-LC3 H1299 cells are treated with 1 μM AZD8055 for 4 h in fed conditions. Cells are then fixed with 4% PFA, and nuclei are stained using 2 μg/ml Hoechst 33342. Fluorescence is analyzed using an imaging cytometer. Cells are considered positive when there are more than four green spots per cell, with a total of 25 fields acquired. The activity of the product is estimated.
Experimental Result Images Methods Biomarkers Images PMID
Immunofluorescence LAMP2A 28498820
Growth inhibition assay Cell viability 28972076
In Vivo
In vivo

SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor.
Animal Research Animal Models Nude mice
Dosages 2 mg/kg
Administration s.c.

Chemical Information & Solubility

Molecular Weight 443.85 Formula

C19H21ClF3N5O2
CAS No. 1523406-39-4 SDF Download SAR405 SDF
Smiles CC1COCCN1C2=CC(=O)N3CCC(N(C3=N2)CC4=CC(=CN=C4)Cl)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 89 mg/mL ( (200.51 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 89 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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