Home PI3K/Akt/mTOR mTOR inhibitor - Apoptosis related activator - Autophagy activator Vistusertib (AZD2014) For research use only.

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. AZD2014 induces proliferation suppression, apoptosis, cell cycle arrest, and autophagy in HCC cells with antitumor activity.

Vistusertib (AZD2014) Chemical Structure

Vistusertib (AZD2014) Chemical Structure

CAS No. 1009298-59-2

Purity & Quality Control

Vistusertib (AZD2014) Related Products

Signaling Pathway

mTOR Signaling Pathways

mTOR Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 Function assay Inhibition of recombinant FLAG-tagged mTOR (1362 to 2549) (unknown origin) expressed in HEK293 cells, IC50 = 0.0028 μM. 23375793
MDA-MB-468 Function assay 2 hrs Inhibition of mTORC2 in human MDA-MB-468 cells assessed as reduction of AKT phosphorylation at Ser473 after 2 hrs, IC50 = 0.08 μM. 23375793
MDA-MB-468 Function assay 2 hrs Inhibition of mTORC1 in human MDA-MB-468 cells assessed as reduction of pS6 phosphorylation at Ser235/236 after 2 hrs, IC50 = 0.2 μM. 23375793
MCF7 Function assay Inhibition of mTORC2 in human MCF7 cells xenografted mouse assessed as modulation substrate 23375793
MCF7 Function assay Inhibition of mTORC1 in human MCF7 cells xenografted mouse assessed as modulation substrate 23375793
MCF7 Cytotoxicity assay 5 days Cytotoxicity against human MCF7 cells after 5 days by Presto blue reagent-based fluorescence analysis ChEMBL
Click to View More Cell Line Experimental Data

Biological Activity

Description 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 proliferation suppression, apoptosis, cell cycle arrest, and autophagy in HCC cells with antitumor activity.
Targets
mTOR [1]
(Cell-free assay)		 P-Akt (S473) [1]
(Cell-free assay)		 pS6 (S235/236) [1]
(Cell-free assay)
2.8 nM 80 nM 200 nM
In vitro
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. [1]
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-4EBP1 / 4EBP1 / p-S6K / S6K / p-AKT S473 / AKT p-mTOR(S2448) / mTOR / p-S6(235/236) / S6 25628925
Immunofluorescence E-cadherin / Vimentin 25628925
Growth inhibition assay Cell viability 26219339
In Vivo
In vivo

AZD2014 induces tumour growth inhibition against several xenograft models including a human primary explant model of ER+ breast cancer. The antitumour activity is associated with modulation of both mTORC1 and mTORC2 substrates. [1]
Animal Research Animal Models Male SCID mice
Dosages 20 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02619864 Completed
Glioblastoma Multiforme
Canadian Cancer Trials Group|AstraZeneca
 December 22 2016 Phase 1
NCT02780830 Withdrawn
Core: Relapsed or Refractory Diffuse Large B-Cell Lymphoma|Module 1: Non-GCB Diffuse Large B-Cell Lymphoma
AstraZeneca
 June 2016 Phase 1
NCT02730923 Active not recruiting
Endometrial Carcinoma|Metastatic Carcinoma|Hormone Receptor Positive Tumor
Centre Leon Berard
 April 2016 Phase 1|Phase 2
NCT02599714 Completed
Advanced and Metastatic Breast Cancer
AstraZeneca
 December 7 2015 Phase 1
NCT02752204 Completed
Diffuse Large B-Cell Lymphoma
University of Birmingham|Bloodwise|AstraZeneca|Cancer Research UK
 October 2015 Phase 2

Chemical Information & Solubility

Molecular Weight 462.54 Formula

C25H30N6O3
CAS No. 1009298-59-2 SDF Download Vistusertib (AZD2014) SDF
Smiles CC1COCCN1C2=NC(=NC3=C2C=CC(=N3)C4=CC(=CC=C4)C(=O)NC)N5CCOCC5C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 92 mg/mL ( (198.9 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
I am looking for a i.p. or i.v. formula of AZD2014. Any suggestion?

Answer:
S2783 AZD2014 can be dissolved in 5% DMSO/30% PEG 300/ddH2O at 5 mg/ml as a clear solution for I.P. use.

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