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 Fórmula: C₂₅H₃₀N₆O₃ Peso molecular: 462.54 Número CE: 682-433-0

GRAU & PUREZA 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

Visão geral

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%

Especificações

Sinónimos

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

Especificações e pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos e fisiológicos

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

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Grau

Moligand™

Tipo de ação

INHIBITOR

Mecanismo de ação

Serine/threonine-protein kinase mTOR inhibitor

Propriedades do produto

ALogP

2.8

Nomes e identificadores

SMILES isoméricas

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

Peso molecular

462.54

Reaxy-Rn

26042180

Reaxys-RN_link_address

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

Alvos associados (humanos)

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)

Propriedades químicas e físicas

• Índice de refração: 1.61