CAS 1123231-07-1|WAY-262611

Introduction:Basic information about CAS 1123231-07-1|WAY-262611, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameWAY-262611
CAS Number1123231-07-1Molecular Weight318.415
Density1.2±0.1 g/cm3Boiling Point544.8±42.0 °C at 760 mmHg
Molecular FormulaC20H22N4Melting Point/
MSDS/Flash Point283.3±27.9 °C

Names

Name1-{1-[4-(2-Naphthyl)-2-pyrimidinyl]-4-piperidinyl}methanamine
SynonymMore Synonyms

WAY-262611 BiologicalActivity

DescriptionWAY-262611 is a wingless β-Catenin agonist that increases bone formation rate with an EC50 of 0.63 μM in TCF-Luciferase assay.
Related CatalogSignaling Pathways >>Stem Cell/Wnt >>β-cateninResearch Areas >>Cancer
Target

EC50: 0.63 μM (β-Catenin)[1]

In VitroWAY-262611 has the most potent activity in the primary assay, low kinase inhibition potential, and high solubility[1].
In VivoWAY-262611 has excellent pharmacokinetic properties and shows a dose dependent increase in the trabecular bone formation rate in ovariectomized rats following oral administration. Calvariae from wt mice treated with WAY-262611 shows statistically increased BFR, while similarly treated KO animals are no different from control. This indicates that WAY-262611 is acting via the Wnt β-catenin pathway and most likely through inhibition of Dkk-1[1].
Animal AdminRats: WAY-262611 is dissolved in DMSO and diluted with saline for iv (Rats). WAY-262611 is prepared in 0.5% methylcellulose/2% Tween-80 for po OVX rats14 are treated orally with 5 (po, vehicle=0.5% methylcellulose/2% Tween-80, qd, 28 days) at four doses. Trabecular bone formation rate (BFR) in the tibia is established in all dose groups at the end of the in-life portion of the study. A clear dose response and activity as low as 0.3 mg/kg/day are observed[1]. Mice: To confirm activity via the Wnt pathway, the calvariae of wild type (wt) and Dkk-1 knockout (KO) mice are treated with 5 once a day for 7 days (DMSO solution, sc injection). The KO animals are not expected to respond because of the inherent inability to inhibit a missing target protein, while wild type animals with fully expressed Dkk-1 are expected to show a pharmacological response [1].
References

[1]. Pelletier JC, et al. (1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases bone formation rate. J Med Chem. 2009 Nov 26;52(22):6962-5.

Chemical & Physical Properties

Density1.2±0.1 g/cm3
Boiling Point544.8±42.0 °C at 760 mmHg
Molecular FormulaC20H22N4
Molecular Weight318.415
Flash Point283.3±27.9 °C
Exact Mass318.184448
PSA55.04000
LogP4.09
Vapour Pressure0.0±1.5 mmHg at 25°C
Index of Refraction1.638
InChIKeyQHLITPHIARVDJI-UHFFFAOYSA-N
SMILESNCC1CCN(c2nccc(-c3ccc4ccccc4c3)n2)CC1
Storage condition2-8℃

Synonyms

1-{1-[4-(2-Naphthyl)-2-pyrimidinyl]-4-piperidinyl}methanamine
4-Piperidinemethanamine, 1-[4-(2-naphthalenyl)-2-pyrimidinyl]-
1-{1-[4-(2-Naphthyl)pyrimidin-2-yl]piperidin-4-yl}methanamine
WAY-262611
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