168425-64-7
Compound 401
CAS: 168425-64-7
Molecular Formula: C16H15N3O2
168425-64-7 - Names and Identifiers
168425-64-7 - Physico-chemical Properties
| Molecular Formula | C16H15N3O2 |
| Molar Mass | 281.31 |
| Density | 1.36±0.1 g/cm3 (20 ºC 760 Torr) |
| Melting Point | 184-186℃ (ethanol ) |
| Boling Point | 456.9±55.0 °C(Predicted) |
| Appearance | powder to crystal |
| Color | White to Light yellow |
| pKa | 1.01±0.20(Predicted) |
| Storage Condition | Store at RT |
| In vitro study | Compound 401 is a potent inhibitor of DNA-PK (IC 50 =0.28 μM). Compound 401 is reported to be a poor inhibitor of PI3K, ATM, and ATR in vitro, but it is active against mTOR. Compound 401 shows activity against mTOR (IC 50 =5.3 μM) but not p110α/p85α PI3K (IC 50 >100 μM). Treatment of cells with Compound 401 blocks the phosphorylation of sites modified by mTOR-Raptor and mTOR-Rictor complexes (ribosomal protein S6 kinase 1 Thr 389 and Akt Ser 473 , respectively). By contrast, there is no direct inhibition of Akt Thr 308 phosphorylation, which is dependent on PI3K. Similar effects are also observed in cells that lack DNA-PK. Compound 401 inhibits immunoprecipitated epitope-tagged mTOR or endogenous mTOR in Raptor immunoprecipitates. In both cases, inhibition of 67% or 78% is obtained at 5 μM or 10 μM Compound 401, respectively. By contrast, dose response curves show that the p110α/p85α or p110β/p85α PI3K complexes are poorly inhibited by Compound 401 at these concentrations. The proliferation of TSC1 -/- fibroblasts is inhibited in the presence of Compound 401, but TSC1 +/+ cells are resistant. |
168425-64-7 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.555 ml | 17.774 ml | 35.548 ml |
| 5 mM | 0.711 ml | 3.555 ml | 7.11 ml |
| 10 mM | 0.355 ml | 1.777 ml | 3.555 ml |
| 5 mM | 0.071 ml | 0.355 ml | 0.711 ml |
Last Update：2024-01-02 23:10:35
168425-64-7 - Reference Information
| biological activity | Compound 401 is a DNA-PK and mTOR inhibitor (IC50 0.28 μm and 5.3 μm, respectively). It had no significant inhibitory effect on p110α/p85α PI3K and inhibited phosphorylation of S6 kinase at Thr389 and phosphorylation of Akt at Ser473 in COS7 cells. |
| Target | Value |
| DNA-PK (Cell-free assay) | 0.28 μM |
| mTOR (Cell-free assay) | 5.3 μM |
Last Update：2024-04-09 21:54:55
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Spot supply
Product Name: Compound 401 Visit Supplier Webpage Request for quotationCAS: 168425-64-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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