Biological Activity
Potent and selective PI 3-kinase β inhibitor (IC50 values are 0.007, 0.1, 3.5 and 5 μM for the β, δ, γ and α isoforms, respectively). Shows >1,000-fold selectively for PI 3-kinase β over a range of other kinases. Inhibits thrombus formation in animal models.
Technical Data
| M. Wt | 364.44 |
| Formula | C21H24N4O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 663619-89-4 |
| PubChem ID | 9907093 |
| InChI Key | CPRAGQJXBLMUEL-UHFFFAOYSA-N |
| Smiles | CC(C1=CC(C)=CN2C(C=C(N3CCOCC3)N=C12)=O)NC4=CC=CC=C4 |
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 | 18.22 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 364.44. 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 | 2.74 mL | 13.72 mL | 27.44 mL |
| 5 mM | 0.55 mL | 2.74 mL | 5.49 mL |
| 10 mM | 0.27 mL | 1.37 mL | 2.74 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.55 mL |
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References
References are publications that support the products' biological activity.
Condliffe et al (2005) Sequential activation of class IB and class IA PI3K is important for the primed respiratory burst of human but not murine neutrophils. Blood 106 1432 PMID: 15878979
Jackson et al (2005) PI 3-kinase p110β: a new target for antithrombotic therapy. Nat.Med. 11 507 PMID: 15834429
Keywords: TGX 221, supplier, TGX221, PI3K, PI, 3-kinase, phosphoinositide, potent, selective, inhibits, inhibitors, beta, β, antithrombotic, PI, 3-Kinase, PI, 3-Kinase, Tocris Bioscience
