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 분자식: C₂₄H₂₉N₇O₅ 분자량: 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

개요

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

동의어

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

사양 및 순도

Moligand™, 10mM in DMSO

생화학 및 생리적 메커니즘

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).

보관 조건

Store at -80°C

배송

Dry ice packs + Cold packs

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등급

Moligand™

작업 유형

INHIBITOR

작동 메커니즘

Inhibitor of mechanistic target of rapamycin kinase

이름과 식별자

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

관련 대상(인간)

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)

화학 및 물리적 특성

• 굴절률: ~1.69
• 끓는점(°C): ~594.2 °C at 760 mmHg