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Vistusertib (AZD2014)

Name: Vistusertib (AZD2014)
Brand: Selleck Chemicals
SKU: S2783
Rating: 5 (86 reviews)

Catalog No.S2783 Purity:99.70%

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

CAS No. 1009298-59-2

Purity & Quality Control

Batch: Purity: 99.70%

99.70

Vistusertib (AZD2014) Related Products

Related Targets	mTORC1 mTORC2	Click to Expand
Related Products	AZD8055 Torin 1 Ridaforolimus (Deforolimus, MK-8669) Sapanisertib (MLN0128) Torkinib (PP242) MHY1485 KU-0063794 Torin 2 OSI-027 WYE-354 WYE-125132 (WYE-132) 3BDO Palomid 529 (P529) Zotarolimus (ABT-578) Salidroside GDC-0349 WAY-600 Onatasertib (CC 223) XL388 WYE-687	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library	Click to Expand

Signaling Pathway

mTOR Signaling Pathway

Cell Data

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

Biological Activity

Description

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
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.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

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.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

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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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