WAY-316606

Cas No.:	915759-45-4
Chemical Name:	WAY-316606,WAY 316606,WAY316606
Synonyms:	WAY-316606,WAY 316606,WAY316606
SMILES:	O=S(C1=CC(S(NC2CCNCC2)(=O)=O)=C(C(F)(F)F)C=C1)(C1=CC=CC=C1)=O
Formula:	C18H19F3N2O4S2
M.Wt:	448.48
Sotrage:	2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO

Description:	WAY 316606 is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC50 of 0.5 μM.
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 EC50 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 (t1/2>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].
In Vitro:	The EC50 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 KD of 0.08 μM and inhibits sFRP-1 with an EC50 of 0.65 μM. WAY-316606 also binds to sFRP-2, albeit over 10 times weaker with a KD 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 IC50 for WAY-316606 is 0.5 μM[2].