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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.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $50 | - | In Stock | |
| 5 mg | $106 | - | In Stock | |
| 10 mg | $179 | - | In Stock | |
| 25 mg | $298 | - | In Stock | |
| 50 mg | $443 | - | In Stock | |
| 100 mg | $655 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $98 | - | In Stock |
| 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 |
| Smiles | C[C@@H]1COCCN1c1cc(=O)n2CC[C@H](N(Cc3cncc(Cl)c3)c2n1)C(F)(F)F |
| Relative Density. | 1.51 g/cm3 (Predicted) |
| Storage | store at low temperature,keep away from direct sunlight | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 27 mg/mL (60.83 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.51 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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