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Technical Data
| Formula | C25H30N6O3 |
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| 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 | |||
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* <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. | ||||||
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| Targets |
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| 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] |
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| 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)
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References
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Customer Product Validation
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Data from [Biochem Biophys Res Commun, 2014, 443(2), 406-12]
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Data from [Biochem Biophys Res Commun, 2014, 443(2), 406-12]
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Data from [Biochem Biophys Res Commun, 2014, 443(2), 406-12]
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Data from [Biochem Biophys Res Commun, 2014, 443(2), 406-12]
Selleck's Vistusertib (AZD2014) has been cited by 89 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 |
| 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 |
| Multifocal Organoid Capturing of Colon Cancer Reveals Pervasive Intratumoral Heterogenous Drug Responses [ Adv Sci (Weinh), 2021, e2103360] | PubMed: 34918496 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.