Vistusertib (AZD2014) - Moligand™, 10mM in DMSO , Serine/threonine-protein kinase mTOR inhibitor, CAS No.1009298-59-2, Serine/threonine-protein kinase mTOR inhibitor

CAS: 1009298-59-2 Cat. No.: V408523 분자식: C₂₅H₃₀N₆O₃ 분자량: 462.54 EC 번호: 682-433-0

등급 & 순도 Moligand™, 10mM in DMSO

Synonyms

3-(2,4-bis((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-N-methylbenzamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

개요

Information

Vistusertib (AZD2014) Vistusertib (AZD2014) is a novel mTOR inhibitor with IC50 of 2.8 nM in a cell-free assay; highly selective against multiple PI3K isoforms (α/β/γ/δ). AZD2014 showed no or weak binding to the majority of kinases when tested at 1 μM.
In vitro

AZD2014 is a close analogue of AZD8055 and a selective inhibitor of mTOR kinase. AZD2014 has greater inhibitory activity against mTORC1 compared to rapamycin: AZD2014 decreases p4EBP1 Thr37/46, inhibits the translation initiation complex and decreases overall protein synthesis while rapamycin has no effect. AZD2014 also inhibits the mTORC2 biomarkers pAKTSer473 and pNDRG1Thr346. AZD2014 has broad antiproliferative activity across multiple tumour cell lines. In particular, AZD2014 induces growth inhibition and cell death in breast cancer cell lines, including ER+ cell lines with acquired resistance to hormone therapy.

In vivo

AZD2014 induces tumour growth inhibition against several xenograft models including a human primary explant model of ER+ breast cancer refractory to tamoxifen. The antitumour activity is associated with modulation of both mTORC1 and mTORC2 substrates.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥97%

사양

동의어

3-(2,4-bis((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-N-methylbenzamide

사양 및 순도

Moligand™, 10mM in DMSO

생화학 및 생리적 메커니즘

Vistusertib (AZD2014) is a novel mTOR inhibitor with IC50 of 2.8 nM in a cell-free assay; highly selective against multiple PI3K isoforms (α/β/γ/δ). AZD2014 showed no or weak binding to the majority of kinases when tested at 1 μM. AZD2014 induces prolifer

보관 조건

Store at -80°C

배송

Dry ice packs + Cold packs

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등급

Moligand™

작업 유형

INHIBITOR

작동 메커니즘

Serine/threonine-protein kinase mTOR inhibitor

제품 특성

ALogP

2.8

이름과 식별자

이성체 SMILES

C[C@H]1COCCN1C2=NC(=NC3=C2C=CC(=N3)C4=CC(=CC=C4)C(=O)NC)N5CCOC[C@@H]5C

분자량

462.54

Reaxy-Rn

26042180

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26042180&ln=

관련 대상(인간)

MTOR Tclin Serine/threonine-protein kinase mTOR (5 Activities)

Discover Target: MTOR

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

화학 및 물리적 특성

• 굴절률: 1.61