product name Vistusertib (AZD2014)
Description: Vistusertib (also known as AZD2014) is a novel, oral mTOR inhibitor with IC50 of 2.8 nM in a cell-free assay; it is highly selective against multiple PI3K isoforms (α/β/γ/δ). It possesses potential antineoplastic activity. AZD2014 enhanced susceptibility of glioblastoma stem-like cells (GSCs) to irradiation both in vitro and under orthotopic in vivo conditions. Kahn J et al pretreated CD133+ and CD15+ GSC cells with AZD2014 (2 µM) for 1 hour, followed by irradiation.
References: Bioorg Med Chem Lett. 2013 Mar 1;23(5):1212-6; Oncotarget. 2014 Jul 15;5(13):4990-5001.
462.54
Formula
C25H30N6O3
CAS No.
1009298-59-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 38 mg/mL (82.15 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
5% DMSO+30% PEG 300+ddH2O: 5mg/mL
Synonyms
other peoduct :
| In Vitro |
Kinase Assay: Cell Assay: 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. |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Bioorg Med Chem Lett. 2013 Mar 1;23(5):1212-6; Oncotarget. 2014 Jul 15;5(13):4990-5001. |
