1. PI3K/Akt/mTOR
    Autophagy
  2. PI3K
    Autophagy

SAR405 

Cat. No.: HY-12481 Purity: 98.48%
Data Sheet SDS Handling Instructions

SAR405 is a PIK3C3/Vps34 inhibitor with an IC50 of 1.2 nM. SAR405 also is a proximal inhibitor of the autophagy machinery.

For research use only. We do not sell to patients.
SAR405 Chemical Structure

SAR405 Chemical Structure

CAS No. : 1523406-39-4

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10 mM * 1 mL in DMSO $151 In-stock
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5 mg $155 In-stock
10 mg $260 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

SAR405 is a PIK3C3/Vps34 inhibitor with an IC50 of 1.2 nM. SAR405 also is a proximal inhibitor of the autophagy machinery.

IC50 & Target

IC50: 1.2 nM (Vps34)[1]
Autophagy[2]

In Vitro

SAR405 is a low-molecular-mass kinase inhibitor of Vps34 (KD 1.5 nM). SAR405 has an exquisite protein and lipid kinase selectivity profile that is explained by its unique binding mode and molecular interactions within the ATP binding cleft of human Vps34. Inhibition of Vps34 kinase activity by SAR405 affects both late endosome-lysosome compartments and prevents autophagy. SAR405 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-1, corresponding to a residence half-life, t1/2, of 3.8 min. The activity of SAR405 is next evaluated on a dedicated Vps34 cellular assay using a GFP-FYVE–transfected HeLa cell line[1]. SAR405 is a PIK3C3/Vps34 inhibitor that prevents autophagy and synergizes with MTOR inhibition in tumor cells. SAR405 is a proximal inhibitor of the autophagy machinery. SAR405 prevents autophagosome formation with an IC50 of 42 nM. Treatment of starved cells with SAR405 completely inhibits the conversion to LC3-II in a dose-dependent manner. The effect of SAR405 on autophagy is then investigated. The GFP-LC3 model is used for the HTS and confirmed its activity on starved cells (IC50=419 nM). The conversion of LC3-I into LC3-II is also analyzed by western blotting on wild-type HeLa and H1299 cells[2].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.2530 mL 11.2651 mL 22.5301 mL
5 mM 0.4506 mL 2.2530 mL 4.5060 mL
10 mM 0.2253 mL 1.1265 mL 2.2530 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

KiNativ profiling is performed. Jurkat cell lysates are treated with 1 μM of SAR405. After 15-min incubation, the desthiobiotin-ATP-acylphosphate probe is added and incubated for 10 min. Samples are prepared for targeted MS analysis. Briefly, samples are prepared for trypsin digestion (denature and then reduce alkylate) and digested with trypsin, and desthiobiotinylated peptides are enriched on streptavidin resin. Enriched probe-labeled peptides are analyzed by LC tandem MS on a Thermo-LTQ ion trap mass spectrometer using proprietary data collection methodology. All quantification is performed by extracting characteristic fragment ion signals from targeted MS/MS spectra and comparing signals in control and treated samples[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

443.85

Formula

C₁₉H₂₁ClF₃N₅O₂

CAS No.

1523406-39-4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 27 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.48%

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Product Name:
SAR405
Cat. No.:
HY-12481
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