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Vistusertib (AZD2014)

Name: Vistusertib (AZD2014)
Brand: Selleck Chemicals
SKU: S2783
Rating: 5 (78 reviews)

Catalog No.S2783

For research use only.

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

Selleck's Vistusertib (AZD2014) has been cited by 78 publications

Purity & Quality Control

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mTOR Signaling Pathway Map

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

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]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

HEK293	NFvneItHfW6ldHnvckBie3OjeR?=		MYfJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IF\MRWcufGGpZ3XkJI1VV1JiKEGzOlIhfG9iMkW0PUkhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iSFXLNlk{KGOnbHzzMEBKSzVyIE2gNE4xODJ6IN88UU4>	MkH4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN\|N{W3PVMoRjJ\|M{e1O\|k{RC:jPh?=
MDA-MB-468	NGHXV4hHfW6ldHnvckBie3OjeR?=	MXSyJIhzew>?	NIrxeWFKdmirYnn0bY9vKG:oIH3UU3JEOiCrbjDoeY1idiCPRFGtUWIuPDZ6IHPlcIx{KGG\|c3Xzd4VlKGG\|IILl[JVkfGmxbjDv[kBCU1RicHjvd5Bpd3K7bHH0bY9vKGG2IGPldlQ4OyCjZoTldkAzKGi{czygTWM2OCB;IECuNFgh\|ryPLh?=	MkLPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN\|N{W3PVMoRjJ\|M{e1O\|k{RC:jPh?=
MDA-MB-468	M1PSbGZ2dmO2aX;uJIF{e2G7	MUeyJIhzew>?	Mn\HTY5pcWKrdHnvckBw\iCvVF;SR\|EhcW5iaIXtZY4hVUSDLV3CMVQ3QCClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gdHM3KHCqb4PwbI9zgWyjdHnvckBifCCVZYKyN\|UwOjN4IHHmeIVzKDJiaILzMEBKSzVyIE2gNE4zKM7:TT6=	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN5NUe5N{c,OjN\|N{W3PVM9N2F-
MCF7	NFi3V2VHfW6ldHnvckBie3OjeR?=		MkHETY5pcWKrdHnvckBw\iCvVF;SR\|IhcW5iaIXtZY4hVUOINzDj[YxteyC6ZX7v[5Ji\nSnZDDtc5V{\SCjc4Pld5Nm\CCjczDtc4R2dGG2aX;uJJN2[nO2cnH0[S=>	MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN5NUe5N{c,OjN\|N{W3PVM9N2F-
MCF7	MlL1SpVv[3Srb36gZZN{[Xl?		M1S1RmlvcGmkaYTpc44hd2ZibWTPVmMyKGmwIHj1cYFvKE2FRkegZ4VtdHNieHXuc4dz[W[2ZXSgcY92e2ViYYPz[ZN{\WRiYYOgcY9lfWyjdHnvckB{fWK\|dILheIU>	NWPmb3JFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzO\|U4QTNpPkKzN\|c2Pzl\|PD;hQi=>
MCF7	NUPsRmN7S3m2b4TvfIlkcXS7IHHzd4F6	MnzYOUBl[Xm\|	MVPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IEWg[IF6eyCkeTDQdoV{fG9iYnz1[UBz\WGpZX70MYJie2WmIH\seY9z\XOlZX7j[UBidmGueYPpdy=>	Mo[5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlM{PjN{NT:nQmNpTU2ETEyvZV4>

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Western blot	p-mTOR(S2448) / mTOR / p-S6(235/236) / S6 ; p-4EBP1 / 4EBP1 / p-S6K / S6K / p-AKT S473 / AKT	26176608 25628925
Immunofluorescence	E-cadherin / Vimentin	25628925
Growth inhibition assay	Cell viability	26219339

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. ^[1]

Protocol (from reference)

References

Solubility (25°C)

In vitro


In vivo	Add solvents to the product individually and in order (Data is from Selleck tests instead of citations): 5% DMSO+30% PEG 300+ddH2O For best results, use promptly after mixing. Click to purchase: PEG300	5mg/mL

Chemical Information

Molecular Weight	462.54
Formula	C₂₅H₃₀N₆O₃
CAS No.	1009298-59-2
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC1COCCN1C2=NC(=NC3=C2C=CC(=N3)C4=CC(=CC=C4)C(=O)NC)N5CCOCC5C

Download Vistusertib (AZD2014) SDF

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.

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02780830	Withdrawn	Drug: AZD2014\|Drug: Ibrutinib	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	Drug: AZD2014\|Drug: Anastrozole	Endometrial Carcinoma\|Metastatic Carcinoma\|Hormone Receptor Positive Tumor	Centre Leon Berard	April 2016	Phase 1\|Phase 2
NCT02619864	Completed	Drug: AZD2014	Glioblastoma Multiforme	Canadian Cancer Trials Group\|AstraZeneca	January 13 2016	Phase 1
NCT02599714	Active not recruiting	Drug: AZD2014\|Drug: Palbociclib\|Drug: Fulvestrant	Advanced and Metastatic Breast Cancer	AstraZeneca	December 7 2015	Phase 1
NCT02752204	Completed	Drug: AZD 2014\|Drug: Rituximab	Diffuse Large B-Cell Lymphoma	University of Birmingham\|Bloodwise\|AstraZeneca\|Cancer Research UK	October 2015	Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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