WYE-354 - Moligand™, 10mM in DMSO , Inhibitor of mechanistic target of rapamycin kinase, CAS No.1062169-56-5, Inhibitor of mechanistic target of rapamycin kinase

CAS: 1062169-56-5 Cat. No.: W407779 Peso molecular: 495.54 PubChem CID: 44219749

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

4-​[6-​[4-​[(methoxycarbonyl)​amino]​phenyl]​-​4-​(4-​morpholinyl)​-​1H-​pyrazolo[3,​4-​d]​pyrimidin-​1-​yl]​-1-​piperidinecarboxylic acid methyl ester

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

WYE-354 WYE-354 is a potent, specific and ATP-competitive inhibitor of mTOR with IC50 of 5 nM, blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) not P-AKT(T308), selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
In vitro

WYE-354 also inhibits several PI3Ks at micromolar levels. In HEK293 cells, WYE-354 (0.2 μM–5 μM) effectively inhibits both mTORC1 and mTORC2. WYE-354 (0.3 μM–10 μM) significantly blocks mTOR signaling and Akt activation in U87MG and MDA361 cells. Furthermore, WYE-354 potently inhibits proliferation in tumor cell lines including MDA-MB-361, MDA-MB-231, MDA-MB-468, LNCap, A498, and HCT116, with IC50 values ranging from 0.28 μM to 2.3 μM. The apoptosis induced by WYE-354 is accompanied by G1 cell cycle arrest and caspases activation. In endothelial HUVEC cells, WYE-354 (10 nM–1 μM) also inhibits both mTORC1 and mTORC2 signaling, as revealed by dephosphorylation of S6 ribosomal protein and Akt, respectively. Furthermore, WYE-354 (10 nM–1 μM) activates mitogen-activated protein kinase (MAPK) signaling, which may be due to its inhibition of mTORC1.

In vivo

In a mice xenograft model of PTEN- PC3MM2 tumor, WYE-354 (50 mg/kg) effectively inhibits mTOR signaling and tumor growth.
Cell Data

cell lines：Ba/F3 cells

Concentrations：0–50 μM, dissolved in DMSO

Incubation Time：72 hours

Powder Purity:≥99%

Specifications

Sinónimos

4-​[6-​[4-​[(methoxycarbonyl)​amino]​phenyl]​-​4-​(4-​morpholinyl)​-​1H-​pyrazolo[3, ​4-​d]​pyrimidin-​1-​yl]​-1-​piperidinecarboxylic acid methyl ester

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

WYE-354 is a potent, specific and ATP-competitive inhibitor of mTOR with IC50 of 5 nM, blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) not P-AKT(T308), selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Inhibitor of mechanistic target of rapamycin kinase

Nombres e identificadores

• Isómeros SMILES: COC(=O)NC1=CC=C(C=C1)C2=NC3=C(C=NN3C4CCN(CC4)C(=O)OC)C(=N2)N5CCOCC5
• PubChem CID: 44219749
• Peso molecular: 495.54

Objetivos asociados (humanos)

MTOR Tclin Serine/threonine-protein kinase mTOR (3 Activities)

Discover Target: MTOR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Índice de refracción: ~1.69
• Punto de ebullición (°C): ~594.2 °C at 760 mmHg