[CAS NO. 1009298-59-2] Vistusertib (AZD2014)
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PRODUCTS SPECIFICATIONS [1009298-59-2]
Store
Catalog
SLK-S2783
Brand
Selleck
CAS
1009298-59-2
DESCRIPTION [1009298-59-2]
Overview
| MDL | MFCD22628784 |
|---|---|
| Molecular Weight | 462.54 |
| Molecular Formula | C25H30N6O3 |
| SMILES | O=C(NC)C1=CC=CC(C2=NC3=NC(N4[C@@H](C)COCC4)=NC(N5[C@@H](C)COCC5)=C3C=C2)=C1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1620 mL | 10.8099 mL | 21.6198 mL |
| 5 mM | 0.4324 mL | 2.1620 mL | 4.3240 mL |
| 10 mM | 0.2162 mL | 1.0810 mL | 2.1620 mL |
| 50 mM | 0.0432 mL | 0.2162 mL | 0.4324 mL |
Description
Vistusertib (AZD2014) is a novel inhibitor with IC50 of 2.8 nM in a cell-free assay; highly selective against multiple 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, , cell cycle arrest, and in HCC cells with antitumor activity.
Targets
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.
References
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