Biological Activity
Inhibitor of DNA-PK, PI 3-kinase (p110α) and mTOR (IC50 values are 2, 8, 20, 26, 48, 83, 88, 150, 850, 920, ~ 1000 and 2300 nM for DNA-PK, p110α, mTORC1, PI 3-KC2β, p110δ, mTORC2, p110β, p110γ, ATR, ATM, PI 3-KC2α and hsVPS34 respectively). Inhibits growth of human tumor xenografts in mice in vivo. Induces autophagosome formation in glioma cells.
Compound Libraries
PI 103 hydrochloride is also offered as part of the Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 384.82 |
| Formula | C19H16N4O3.HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 371935-79-4 |
| PubChem ID | 16739368 |
| InChI Key | XSQMYBFFYPTMFE-UHFFFAOYSA-N |
| Smiles | OC1=CC(C(N=C4N5CCOCC5)=NC3=C4OC2=NC=CC=C23)=CC=C1.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 7.7 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 384.82. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.6 mL | 12.99 mL | 25.99 mL |
| 5 mM | 0.52 mL | 2.6 mL | 5.2 mL |
| 10 mM | 0.26 mL | 1.3 mL | 2.6 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
Molarity Calculator
Reconstitution Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
Fan et al (2006) A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer cell 9 341 PMID: 16697955
Knight et al (2006) A pharmacological map of the PI3-K family defines a role for p110α in insulin signaling. Cell 125 733 PMID: 16647110
Raynaud et al (2007) Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositol 3-kinase. Cancer Res. 67 5840 PMID: 17575152
Fan et al (2010) Akt and autophagy cooperate to promote survival of drug-resistant glioma. Sci.Signal. 3 ra81 PMID: 21062993
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