SAR405
CAS No. : 1523406-39-4
| Size | Price | Stock |
|---|---|---|
| 2mg | $90 | In-stock |
| 5mg | $130 | In-stock |
| 10mg | $230 | In-stock |
| 25mg | $460 | In-stock |
| 50mg | $690 | In-stock |
| 100mg | $1035 | In-stock |
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| 500 mg | Get quote | |
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| Cat. No. : | HY-12481 |
| M.Wt: | 443.85 |
| Formula: | C19H21ClF3N5O2 |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 27 mg/mL;H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) |
SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity[1][2].
IC50 & Target: IC50: 1.2 nM (Vps34)[1]
Kd: 1.5 nM (Vps34)[1]
Autophagy[2]
In Vitro: The activity of SAR405 is next evaluated on a dedicated Vps34 cellular assay using a GFP-FYVE–transfected HeLa cell line[1].
SAR405 prevents autophagy and synergizes with mTOR inhibition in tumor cells. 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].
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