[CAS NO. 915759-45-4] WAY 316606
PRODUCTS SPECIFICATIONS [915759-45-4]
DESCRIPTION [915759-45-4]
Overview
| MDL | MFCD18206894 |
|---|---|
| Molecular Weight | 448.48 |
| Molecular Formula | C18H19F3N2O4S2 |
| SMILES | O=S(C1=CC(S(=O)(C2=CC=CC=C2)=O)=CC=C1C(F)(F)F)(NC3CCNCC3)=O |
2 Publications Citing Use of MCE
Summary
IC50 & Target
IC50: 0.5 μM (sFRP-1) [1]
In Vitro
The EC 50 of WAY-316606 for Wnt-Luciferase Activity from U2-OS Cells is 0.65 μM [1] . WAY-316606 binds to secreted frizzled-related protein (sFRP)-1 inhibitor with a K D of 0.08 μM and inhibits sFRP-1 with an EC 50 of 0.65 μM. WAY-316606 also binds to sFRP-2, albeit over 10 times weaker with a K D of 1 μM. Using a fluorescence polarization binding assay that employs a fluorescent probe compound and purified human sFRP-1 protein in a competitive-binding format, the IC 50 for WAY-316606 is 0.5 μM [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
WAY-316606 increases bone formation when tested in a neonatal murine calvarial assay. WAY-316606 increases total bone area up to 60% in a dose-dependent manner with an EC 50 of about 1 nM. WAY-316606 has good aqueous solubility, moderate to low inhibition of cytochrome p450 isozymes (3A4, 2D6, 2C9) and good stability in rat and human liver microsomes (t 1/2 >60 min in each species). In female Sprague-Dawley rats, WAY-316606 exhibits high plasma clearance (77 mL/min/kg, greater than hepatic blood flow) following a single intravenous bolus dose (2 mg/kg), which results in a rapid decline of drug exposure in the plasma despite the route of administration [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 : ≥ 100 mg/mL ( 222.98 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2298 mL | 11.1488 mL | 22.2975 mL |
| 5 mM | 0.4460 mL | 2.2298 mL | 4.4595 mL |
| 10 mM | 0.2230 mL | 1.1149 mL | 2.2298 mL |
References
- [1] Moore, WJ, et al. Modulation of Wnt Signaling Through Inhibition of Secreted Frizzled-Related Protein I (sFRP-1) with N-Substituted Piperidinyl Diphenylsulfonyl Sulfonamides. Journal of Medicinal Chemistry (2009), 52(1), 105-116.
- [2] Bodine PV, et al. A small molecule inhibitor of the Wnt antagonist secreted frizzled-related protein-1 stimulates bone formation. Bone. 2009 Jun;44(6):1063-8.