Vistusertib (AZD2014)

Catalog No.S2783

Vistusertib (AZD2014) Chemical Structure

Molecular Weight(MW): 462.54

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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USD 270 In stock

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10 Customer Reviews

  • Murine macrophages were treated with AZD2014 (10 nm) or rapamycin (10 ng/ml) for the time periods indicated. B, immunoblot analysis of whole cell lysate performed using an antibody detecting total ERK and phospho-ERK (Thr202/Tyr204). C, detection of MKP-1. Immunoblot analysis of whole cell lysate performed using an antibody against MKP-1 and β-actin.

    J Biol Chem 2013 288(47), 33966-77. Vistusertib (AZD2014) purchased from Selleck.

    Tumor growth inhibition studies were performed in SCID mice. Mice bearing 300 mm3 tumors were randomly divided into two groups and were treated with 5 mg/kg AZD-2014 (PO, QD x 14; n = 10, the dose was based on results from pre-experiments) or vehicle (saline, PO, QD x 14; n = 10). After AZD-2014 administration, tumor tissues were isolated and lysed, activation of Akt and mTORC1/2 was tested by Western blot.

    Biochem Biophys Res Commun, 2014, 443(2): 406-12. Vistusertib (AZD2014) purchased from Selleck.

  • Biochem Biophys Res Commun 2014 443(2), 406-12. Vistusertib (AZD2014) purchased from Selleck.

    Biochem Biophys Res Commun 2014 443(2), 406-12. Vistusertib (AZD2014) purchased from Selleck.

  • Biochem Biophys Res Commun 2014 443(2), 406-12. Vistusertib (AZD2014) purchased from Selleck.

    Biochem Biophys Res Commun 2014 443(2), 406-12. Vistusertib (AZD2014) purchased from Selleck.

  • HT-29 cells were treated with vehicle or AZD-2014 (50 nM) for 72 h, cell cycle distribution was analyzed by FACS.

    Biochem Biophys Res Commun 2014 443, 406-12. Vistusertib (AZD2014) purchased from Selleck.

    HT-29 cells were treated with vehicle ("Ctrl") or different concentrations of AZD-2014 for 72 h.

    Biochem Biophys Res Commun 2014 443, 406-12. Vistusertib (AZD2014) purchased from Selleck.

  • Autophagy in NCI-H460 (C, D) and NCI-H460/R (E, F) cells was assessed by fluorescence microscopy. Cells were stained with acridine orange to detect the presence of acidic autophagosomes (acridin orange shifts its fluorescence emission from green to red when found in acidic compartments). Nuclei were counterstained with Hoechst 33342 (blue). Number of autophagosomes increased in NCI-H460 cells (D) after 18 h of 250 nM ADZ2014 treatment, in comparison with untreated cells (C). NCI-H460/R cells treated with 100 nM AZD2014 for 18 h also showed increased number of autophagosomes in the cytoplasm (F) when compared to untreated cells (E).

    2013 Dr. Milica Pesic from Institute for Biological Research. Vistusertib (AZD2014) purchased from Selleck.

    The effects of SelleckChem inhibitors on sea urchin embryo development evaluated 24 h after fertilization. All compounds were added to embryos suspension 20 min after fertilization. The relative presence of late gastrula, swimming blastula, undeveloped embryos and dead embryos was compared next to untreated control embryos (A). Fertilized egg, swimming blastula and late gastrula are illustrated (B). The embryonic development was relatively synchronized in untreated control samples after 24 h (A, E). GSK690693 treatment sustained the development of embryos. Swimming blastulas kept normal motility regardless the deformities in their shape. Tipifarnib treatment induced significant toxicity due to occurrence of dead fragmented embryos. Some abnormal blastulas kept the motility. AZD2014 treatment sustained the development of embryos. Some developed gastrulas and blastulas were less motile in comparison with control (A, C). WZ811 was the least toxic compound. Significant number of gastrulas and blastulas was developed. However, their motility was considerably suppressed (A, D). In contrast to SelleckChem inhibitors, classic anticancer agent – cisplatin was extremely toxic to sea urchin embryos (A). Cisplatin killed many embryos, while a small amount of survived embryos was stopped at early phases of development: immediately after fertilization or after first and second division (A, F).

    2013 Dr. Milica Pesic from Institute for Biological Research. Vistusertib (AZD2014) purchased from Selleck.

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Biological Activity

Description 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)
PI3Kα [2]
2.8 nM 80 nM 200 nM 3.766 μM
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 MkfmSpVv[3Srb36gZZN{[Xl? NHz3dXFKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JGZNSUdvdHHn[4VlKG2WT2KgLFE{PjJidH:gNlU1QSliKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{NCCLQ{WwQVIvQCCwTR?= NVjCcIx5OjN|N{W3PVM>
human MDA-MB-468 cells NInXfoNHfW6ldHnvckBie3OjeR?= MWmyJIg> MoLUTY5pcWKrdHnvckBw\iCvVF;SR|IhcW5iaIXtZY4hVUSDLV3CMVQ3QCClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gRWtVKHCqb4PwbI9zgWyjdHnvckBifCCVZYK0O|Mh[W[2ZYKgNkBpenNuIFnDOVA:OC5yODFOwG0> MlK0NlM{PzV5OUO=
human MDA-MB-468 cells M4TReWZ2dmO2aX;uJIF{e2G7 MnrpNkBp M4LHT2lvcGmkaYTpc44hd2ZibWTPVmMyKGmwIHj1cYFvKE2GQT3NRk01PjhiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJJBUPiCyaH;zdIhwenmuYYTpc44h[XRiU3XyNlM2NzJ|NjDh[pRmeiB{IHjyd{whUUN3ME2wMlIh|ryP MnvnNlM{PzV5OUO=
human MCF7 cells MWfGeY5kfGmxbjDhd5NigQ>? MXzJcohq[mm2aX;uJI9nKG2WT2LDNUBqdiCqdX3hckBOS0Z5IHPlcIx{KHinbn;ndoFnfGWmIH3veZNmKGG|c3Xzd4VlKGG|IH3v[JVt[XSrb36gd5Vje3S{YYTl MYmyN|M4PTd7Mx?=

... Click to View More Cell Line Experimental Data

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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 5% DMSO+30% PEG 300+ddH2O 5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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 Conditions Sponsor/Collaborators Start Date Phases
NCT02831257 Recruiting Neurofibromatosis 2|Meningioma Massachusetts General Hospital|AstraZeneca|United States Department of Defense July 2016 Phase 2
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
NCT02813135 Recruiting Children, Adolescents and Young Adults With Refractory or Recurrent Malignancies Gustave Roussy, Cancer Campus, Grand Paris|National Cancer Institute, France June 2016 Phase 1|Phase 2
NCT02730923 Recruiting Endometrial Carcinoma|Metastatic Carcinoma|Hormone Receptor Positive Tumor Centre Leon Berard April 2016 Phase 1|Phase 2
NCT02640755 Active, not recruiting Solid Malignancies AstraZeneca|Quintiles, Inc. January 2016 Phase 1
NCT02599714 Recruiting Advanced and Metastatic Breast Cancer AstraZeneca|SCRI Development Innovations, LLC December 2015 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID