SAR405

For research use only.

Catalog No.S7682

14 publications

SAR405 Chemical Structure

CAS No. 1523406-39-4

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.

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10mM (1mL in DMSO) USD 259 In stock
USD 170 In stock
USD 570 In stock
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Selleck's SAR405 has been cited by 14 publications

1 Customer Review

  • RT-112 and RT-112 (CisPt-R) cells were treated with cisplatin, SAR405, and a combination of both in absence and presence of QVD (10 µM). Again, the concentrations used were the IC50 or half IC50 values for RT-112 (CisPt-R) and RT-112, respectively. After 48 hours, the cells were lysed, and cleared cellular lysates were subjected to SDS-PAGE and immunoblotting for PARP, caspase-3 (Casp3), and Actin. One representative immunoblot is shown.

    Urol Oncol, 2018, 36(4):160.e1-160.e13. SAR405 purchased from Selleck.

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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

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].

Assay
Methods Test Index PMID
Immunofluorescence
LAMP2A; 

PubMed: 28498820     


Exogenously supplied CholEsteryl-BODIPY (1ug/ml; 4 hours) accumulates in distinctive puncta in siRNA-control Tsc2-/- MEFs pretreated with CQ (5uM) or SAR405 (1uM) for 16 hours. siRNA-Ldlr transfected Tsc2- /- MEF pretreated with CQ show no accumulation of exogenous cholesterol esters.

28498820
Growth inhibition assay
Cell viability ; 

PubMed: 28972076     


SAR405 reduces HNSCC proliferation with IC50=7.92 μM over 72 h, graph depicts three experiments plated in triplicate.

28972076

Protocol

Cell Research:

[1]

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  • 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 hydroxychloroquine with Vps34 compound or DMSO. For mTOR inhibitor, GFP-LC3 H1299 cells are treated with 1 μM AZD8055 for 4 h in fed conditions (DMEM, 10% FCS, 1 mM L-glutamine with SAR405 or DMSO. 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.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 88 mg/mL warmed (198.26 mM)
Ethanol 88 mg/mL (198.26 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
4mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 443.85
Formula

C19H21ClF3N5O2

CAS No. 1523406-39-4
Storage powder
in solvent
Synonyms N/A
Smiles CC1COCCN1C2=CC(=O)N3CCC(N(C3=N2)CC4=CC(=CN=C4)Cl)C(F)(F)F

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID