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Vistusertib (AZD2014) mTOR inhibitor

Name: Vistusertib (AZD2014)
Brand: Selleck Chemicals
SKU: S2783
Availability: InStock
Rating: 5 (91 reviews)

Cat.No.S2783

Vistusertib (AZD2014) is a novel mTOR inhibitor with IC50 of 2.8 nM in a cell-free assay, and is highly selective against multiple PI3K isoforms (α/β/γ/δ). It showed no or weak binding to the majority of kinases when tested at 1 μM. This compound induces proliferation suppression, apoptosis, cell cycle arrest, and autophagy in HCC cells with antitumor activity.

Chemical Structure

Molecular Weight: 462.54

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Quality Control

Batch: Purity: 99.70%

99.70

Related Targets	PI3K Akt GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PI4K PP2A
Other mTOR Inhibitors	Torin 1 Torin 2 AZD8055 Ridaforolimus (Deforolimus, MK-8669) Sapanisertib (MLN0128, INK-128) Torkinib (PP242) MHY1485 KU-0063794 OSI-027 3BDO

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	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

Solubility

In vitro
Batch:

DMSO : 92 mg/mL (198.9 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 30%PEG300 2 65%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (10.81mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 300 μL of PEG 300, mix evenly to clarify it; then continue to add 650 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	462.54	Formula	C₂₅H₃₀N₆O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1009298-59-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			SMILES	CC1COCCN1C2=NC(=NC3=C2C=CC(=N3)C4=CC(=CC=C4)C(=O)NC)N5CCOCC5C

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	mTOR (Cell-free assay) 2.8 nM P-Akt (S473) (Cell-free assay) 80 nM pS6 (S235/236) (Cell-free assay) 200 nM
In vitro	Vistusertib (AZD2014) is a close analogue of AZD8055 and a selective inhibitor of mTOR kinase. It has greater inhibitory activity against mTORC1 compared to rapamycin: this compound decreases p4EBP1 Thr37/46, inhibits the translation initiation complex and decreases overall protein synthesis while rapamycin has no effect. It also inhibits the mTORC2 biomarkers pAKTSer473 and pNDRG1Thr346. AZD2014 has broad antiproliferative activity across multiple tumour cell lines. In particular, it induces growth inhibition and cell death in breast cancer cell lines, including ER+ cell lines with acquired resistance to hormone therapy.
In vivo	Vistusertib (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.
References	[1] http://cancerres.aacrjournals.org/cgi/content/short/72/8_MeetingAbstracts/917?rss=1 [2] https://pubmed.ncbi.nlm.nih.gov/26358751/

Applications

Methods	Biomarkers	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

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-07-10)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02813135	RECRUITING	Pediatric Cancer	Gustave Roussy, Cancer Campus, Grand Paris	2016-08-03	PHASE1; PHASE2
NCT02208375	ACTIVE_NOT_RECRUITING	BRCA1 Mutation Carrier; BRCA2 Mutation Carrier; Endometrial Adenocarcinoma; Estrogen Receptor Negative; HER2/Neu Negative; High Grade Ovarian Serous Adenocarcinoma; Progesterone Receptor Negative; Recurrent Breast Carcinoma; Recurrent Fallopian Tube Carcinoma; Recurrent Ovarian Carcinoma; Recurrent Primary Peritoneal Carcinoma; Recurrent Uterine Corpus Carcinoma; Stage III Uterine Corpus Cancer AJCC v7; Stage IV Breast Cancer AJCC v6 and v7; Stage IV Uterine Corpus Cancer AJCC v7; Triple-Negative Breast Carcinoma	M.D. Anderson Cancer Center	2014-11-11	PHASE1
NCT03334617	ACTIVE_NOT_RECRUITING	Non-Small Cell Lung Cancer	AstraZeneca	2017-12-18	PHASE2
NCT02398747	COMPLETED	Advanced Solid Malignancies	AstraZeneca	2015-03-17	PHASE1
NCT02664935	COMPLETED	Non-Small Cell Lung Cancer; Carcinoma, Squamous Cell; Adenocarcinoma	University of Birmingham	2015-05-13	PHASE2
NCT02299999	ACTIVE_NOT_RECRUITING	Metastatic Breast Cancer	UNICANCER	2014-04-07	PHASE2

Tech Support

Handling Instructions

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Frequently Asked Questions

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

Answer:
It 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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