[CAS NO. 850717-64-5] BX517
PRODUCTS SPECIFICATIONS [850717-64-5]
DESCRIPTION [850717-64-5]
Overview
| MDL | MFCD28044315 |
|---|---|
| Molecular Weight | 282.30 |
| Molecular Formula | C15H14N4O2 |
| SMILES | NC(NC1=CC=C(NC(/C2=C(C)\C3=CC=CN3)=O)C2=C1)=O |
1 Publications Citing Use of MCE
Summary
BX517 is a potent and selective inhibitor of PDK1 with IC 50 of 6 nM.
IC50 & Target
IC50: 6 nM (PDK1)
In Vitro
BX-517 blocks activation of Akt in tumor cells, is potent with IC 50 of 0.1-1.0 μM [1] . BX-517 blocks AKT2 activation in cells with submicromolar potency. BX-517 is 100-fold selective or better against a panel of seven additional Ser/Thr and Tyr kinases [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 27 mg/mL ( 95.64 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.5423 mL | 17.7117 mL | 35.4233 mL |
| 5 mM | 0.7085 mL | 3.5423 mL | 7.0847 mL |
| 10 mM | 0.3542 mL | 1.7712 mL | 3.5423 mL |
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1.
References
- [1] Islam I, et al. Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3819-25.
- [2] Islam I, et al. Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3814-8.