Vistusertib (AZD2014)

Catalog No.S2783 Batch:S278303

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Technical Data

Formula

C25H30N6O3
Molecular Weight 462.54 CAS No. 1009298-59-2
Solubility (25°C)* In vitro DMSO 92 mg/mL (198.9 mM)
Water Insoluble
Ethanol Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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. AZD2014 induces proliferation suppression, apoptosis, cell cycle arrest, and autophagy in HCC cells with antitumor activity.
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]
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]

Protocol (from reference)

Animal Study:

[2]
  • Animal Models

    Male SCID mice

  • Dosages

    20 mg/kg

  • Administration

    p.o.

Customer Product Validation

Data from [Biochem Biophys Res Commun, 2014, 443(2), 406-12]

Data from [Biochem Biophys Res Commun, 2014, 443(2), 406-12]

Data from [Biochem Biophys Res Commun, 2014, 443(2), 406-12]

Data from [Biochem Biophys Res Commun, 2014, 443(2), 406-12]

Selleck's Vistusertib (AZD2014) has been cited by 90 publications

USP9X mediates an acute adaptive response to MAPK suppression in pancreatic cancer but creates multiple actionable therapeutic vulnerabilities [ Cell Rep Med, 2023, 4(4):101007] PubMed: 37030295
m7G-related genes predict prognosis and affect the immune microenvironment and drug sensitivity in osteosarcoma [ Front Pharmacol, 2023, 14:1158775] PubMed: 37654606
Co-Targeting FASN and mTOR Suppresses Uveal Melanoma Growth [ Cancers (Basel), 2023, 15(13)3451] PubMed: 37444561
Co-Targeting FASN and mTOR Suppresses Uveal Melanoma Growth [ Cancers (Basel), 2023, 15(13)3451] PubMed: 37444561
Drug-Dependent Morphological Transitions in Spherical and Worm-Like Polymeric Micelles Define Stability and Pharmacological Performance of Micellar Drugs [ Small, 2022, 18(4):e2103552] PubMed: 34841670
High-risk neuroblastoma with NF1 loss of function is targetable using SHP2 inhibition [ Cell Rep, 2022, 40(4):111095] PubMed: 35905710
Reciprocal effects of mTOR inhibitors on pro-survival proteins dictate therapeutic responses in tuberous sclerosis complex [ iScience, 2022, 25(11):105458] PubMed: 36388985
Culture and multiomic analysis of lung cancer patient-derived pleural effusions revealed distinct druggable molecular types [ Sci Rep, 2022, 12(1):6345] PubMed: 35428753
[The dual mTORC1/2 inhibitor AZD2014 inhibits acute graft rejection in a rat liver transplantation model] [ Nan Fang Yi Ke Da Xue Xue Bao, 2022, 42(4):598-603] PubMed: 35527497
SARS-CoV-2 infection rewires host cell metabolism and is potentially susceptible to mTORC1 inhibition [ Nat Commun, 2021, 12(1):1876] PubMed: 33767183

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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