475986

mTOR Kinase Inhibitor II, WYE-354

The mTOR Kinase Inhibitor II, WYE-354, also referenced under CAS 1062169-56-5, controls the biological activity of mTOR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonyme(s) : mTOR Kinase Inhibitor II, WYE-354, Methyl-4-(6-{4-[(methoxycarbonyl)amino]phenyl}-4-morpholin-4-yl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate, mTOR Inhibitor II
• Formule empirique (notation de Hill) : C₂₄H₂₉N₇O₅
• Numéro CAS: 1062169-56-5
• Poids moléculaire : 495.53
• Numéro MDL: MFCD18074514
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Essai: ≥98% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: white
• Solubilité: DMSO: 50 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C
• Chaîne SMILES: N5(CCOCC5)c1nc(nc3c1C=[N]#[N]3C4CCN(CC4)C(=O)OC)c2ccc(cc2)NC(=O)OC
• InChI: 1S/C24H29N7O5/c1-34-23(32)26-17-5-3-16(4-6-17)20-27-21(29-11-13-36-14-12-29)19-15-25-31(22(19)28-20)18-7-9-30(10-8-18)24(33)35-2/h3-6,15,18H,7-14H2,1-2H3,(H,26,32)
• Clé InChI: IMXHGCRIEAKIBU-UHFFFAOYSA-N

Description

Description générale

A cell-permeable pyrazolopyrimidine compound that acts as a potent and ATP-competitive mTOR inhibitor (IC₅₀ = 5 nM with S6K as the substrate and 100 µM ATP) with much reduced activity against PI 3-Kα or PI 3-Kγ (IC₅₀ = 1.89 and 7.37 µM, respectively) and little or no activity toward 24 other kinases (IC₅₀ >50 µM). WYE-354 is equally potent against mTORC1 and mTORC2 activities in HEK293 immune complex kinase assays using S6K and Akt as the respective substrate (IC₅₀<200 nM; [ATP] = 100 µM) and effectively blocks cellular phosphorylation of S6K on T389 and Akt on S473 both in cultures and in a murine xenograft model, resulting in a significant suppression of PC3MM2-derived tumor growth (by 86% on day 7; 50 mg/kg, i.p twice per day) in vivo.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Autres remarques

Yu, K., et al. 2009. Cancer Res.69, 6232.
Zask, A., et al. 2009. J. Med. Chem.52, 5013.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 2
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable