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475986 mTOR Kinase Inhibitor II, WYE-354 - CAS 1062169-56-5 - Calbiochem

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.

Ficha de datos de seguridad (MSDS o SDS), certificado de análisis y de calidad (CoA y CoQ), expedientes, folletos y otros documentos disponibles.

Sinónimos: 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

475986
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Descripción

Replacement Information

Tabla espec. clave

CAS #Empirical Formula
1062169-56-5C₂₄H₂₉N₇O₅

Products

Número de referenciaEmbalaje Cant./Env.
475986-5MG Ampolla de plást. 5 mg
Description
OverviewA 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.
Catalogue Number475986
Brand Family Calbiochem®
SynonymsMethyl-4-(6-{4-[(methoxycarbonyl)amino]phenyl}-4-morpholin-4-yl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate, mTOR Inhibitor II
References
ReferencesYu, K., et al. 2009. Cancer Res. 69, 6232.
Zask, A., et al. 2009. J. Med. Chem. 52, 5013.
Product Information
CAS number1062169-56-5
FormWhite solid
Hill FormulaC₂₄H₂₉N₇O₅
Chemical formulaC₂₄H₂₉N₇O₅
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Número de referencia GTIN
475986-5MG 04055977184389

Documentation

mTOR Kinase Inhibitor II, WYE-354 - CAS 1062169-56-5 - Calbiochem Ficha datos de seguridad (MSDS)

Título

Ficha técnica de seguridad del material (MSDS) 

mTOR Kinase Inhibitor II, WYE-354 - CAS 1062169-56-5 - Calbiochem Certificados de análisis

CargoNúmero de lote
475986

Referencias bibliográficas

Visión general referencias
Yu, K., et al. 2009. Cancer Res. 69, 6232.
Zask, A., et al. 2009. J. Med. Chem. 52, 5013.
Ficha técnica

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision17-September-2010 RFH
SynonymsMethyl-4-(6-{4-[(methoxycarbonyl)amino]phenyl}-4-morpholin-4-yl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate, mTOR Inhibitor II
DescriptionA 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.
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1062169-56-5
Chemical formulaC₂₄H₂₉N₇O₅
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesYu, K., et al. 2009. Cancer Res. 69, 6232.
Zask, A., et al. 2009. J. Med. Chem. 52, 5013.