Vistusertib (AZD2014)

Catalog No.S2783

Vistusertib (AZD2014) Chemical Structure

Molecular Weight(MW): 462.54

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.

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Cited by 38 Publications

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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.
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 cells M2\afGZ2dmO2aX;uJIF{e2G7 M{e1c2lvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgSmxCTy22YXfn[YQhdVSRUjCoNVM3OiC2bzCyOVQ6MSBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDISWszQTNiY3XscJMtKEmFNUC9Nk45KG6P MUiyN|M4PTd7Mx?=
human MDA-MB-468 cells NV;jNVFETnWwY4Tpc44h[XO|YYm= M{fpOlIhcA>? NYD2eVVYUW6qaXLpeIlwdiCxZjDtWG9TSzJiaX6gbJVu[W5iTVTBMW1DNTR4ODDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhSUuWIIDoc5NxcG:{eXzheIlwdiCjdDDT[ZI1PzNiYX\0[ZIhOiCqcoOsJGlEPTB;MD6wPEDPxE1? NX;CRlQ6OjN|N{W3PVM>
human MDA-MB-468 cells NHHxZ|RHfW6ldHnvckBie3OjeR?= NV\Id3h5OiCq Ml21TY5pcWKrdHnvckBw\iCvVF;SR|EhcW5iaIXtZY4hVUSDLV3CMVQ3QCClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gdHM3KHCqb4PwbI9zgWyjdHnvckBifCCVZYKyN|UwOjN4IHHmeIVzKDJiaILzMEBKSzVyPUCuNkDPxE1? MWSyN|M4PTd7Mx?=
human MCF7 cells MlXaSpVv[3Srb36gZZN{[Xl? NFz4UohKdmirYnn0bY9vKG:oIH3UU3JEOSCrbjDoeY1idiCPQ1[3JINmdGy|IIjlco9oemGodHXkJI1wfXOnIHHzd4V{e2WmIHHzJI1w\HWuYYTpc44he3Wkc4TyZZRm NUTLTY9[OjN|N{W3PVM>

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-4EBP1 / 4EBP1 / p-S6K / S6K / p-AKT S473 / AKT; 

PubMed: 25628925     


Biochemical activity of AZD2014 and rapamycin in blocking mTORC1 and mTORC2 signaling. HCC cells were treated with DMSO or increasing concentrations of AZD2014 or rapamycin for 1 hour before lysis and immunoblotting.

p-mTOR(S2448) / mTOR / p-S6(235/236) / S6; 

PubMed: 26176608     


AZD2014 and rapamycin inhibited mTOR signaling in A549 cells as shown by the decreased phosphorylation of mTORand S6 after treatment for 24h.

25628925 26176608
Immunofluorescence
E-cadherin / Vimentin ; 

PubMed: 25628925     


Immunofluorescence staining in Huh-7 and SMMC-7721 cells. bars, 30 μm

25628925
Growth inhibition assay
Cell viability; 

PubMed: 26219339     


Dose-response curve for AZD2014 was determined for NF2-deficient primary (MN521, MN527, MN580) and immortalized (Ben-Men-1) meningioma cells lines, as well as primary (AC028) and immortalized arachnoid (AC007) cell lines. AZD2014 in a 10 point, 4-fold serial dilution series (0-20μM).

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

Solubility (25°C)

In vitro DMSO 38 mg/mL (82.15 mM)
Water Insoluble
Ethanol Insoluble
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. 		5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 462.54
Formula

C25H30N6O3
CAS No. 1009298-59-2
Storage powder
in solvent
Synonyms N/A

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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 Recruiting Drug: AZD2014|Drug: Anastrozole Endometrial Carcinoma|Metastatic Carcinoma|Hormone Receptor Positive Tumor Centre Leon Berard April 2016 Phase 1|Phase 2
NCT02619864 Active not recruiting 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 Active not recruiting Drug: AZD 2014|Drug: Rituximab Diffuse Large B-Cell Lymphoma University of Birmingham|Bloodwise|AstraZeneca|Cancer Research UK October 2015 Phase 2

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

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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.

selleck catalog

mTOR Signaling Pathway Map

mTOR Inhibitors with Unique Features

  • Pan mTOR inhibitor

    KU-0063794 : mTORC1 and mTORC2, IC50=~10 nM.

  • Most Potent mTOR Inhibitor

    Rapamycin (Sirolimus) : mTOR, IC50=~0.1 nM.

  • FDA-approved mTOR Inhibitor

    Temsirolimus (CCI-779, NSC 683864) : Approved by FDA for Renal Cell Carcinoma (RCC).

  • Newest mTOR Inhibitor

    XL388 New : Highly potent, selective, ATP-competitive inhibitor of mTOR with IC50 of 9.9 nM, 1000-fold selectivity over the closely related PI3K kinases.

Related mTOR Products

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  • Dorsomorphin (Compound C) New

    Dorsomorphin is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type I BMP receptor activity.

  • Rapamycin (Sirolimus)

    Rapamycin (Sirolimus) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.

  • Everolimus (RAD001)

    Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay.

  • AZD8055

    AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM in MDA-MB-468 cells with excellent selectivity (∼1,000-fold) against PI3K isoforms and ATM/DNA-PK. Phase 1.

    Features:First drug to inhibit both types of mTOR protein.

  • Torin 1

    Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM in cell-free assays; exhibits 1000-fold selectivity for mTOR than PI3K.

  • Temsirolimus (CCI-779, NSC 683864)

    Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay.

  • Sapanisertib (INK 128, MLN0128,TAK-228)

    Sapanisertib (INK 128, MLN0128) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1.

  • Tacrolimus (FK506)

    Tacrolimus (FK506) is a 23-membered macrolide lactone, it reduces peptidyl-prolyl isomerase activity in T cells by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID