AZD2014 |
AZD2014 : ATP competitive inhibitor of MTOR
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| MTOR |
|
|
ATP competitive
10 nM - 2 uM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
The activity of the lipid kinases, class I PI3Ks α, β, γ, δ was measured with the lipid PIP2 as subs ...
Potency Cellular
In Vitro
MTOR
Mode of Action: ATP competitive
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1158/1535-7163.MCT-15-0365
In Vivo Validations
Rat, Mouse
Dose: 4 uM/kg (rat), 7.5-15 mg/kg (mouse)
Route of delivery:
Intravenous, Oral
Systemic clearance:
12.6 mL/min/kg (rat), 10.4 (mouse)
Organ of interest (O):
MCF7 xenograft
Target engagement assay:
In xenografts, AZD2014 dose-dependently decrease protein-substrate phosphorylation (S6 and AKT).
DOI Reference: 10.1158/1535-7163.MCT-15-0365
Chemical Information
| Molecular Formula | C25H30N6O3 |
| SMILEs | CNC(=O)c1cccc(-c2ccc3c(N4CCOC[C@@H]4C)nc(N4CCOC[C@@H]4C)nc3n2)c1 |
| InChI | InChI=1S/C25H30N6O3/c1-16-14-33-11-9-30(16)23-20-7-8-21(18-5-4-6-19(13-18)24(32)26-3)27-22(20)28-25(29-23)31-10-12-34-15-17(31)2/h4-8,13,16-17H,9-12,14-15H2,1-3H3,(H,26,32)/t16-,17-/m0/s1 |
| Molecular weight | 462.24 Da |
| AlogP | 0.0 |
| HBond acceptors | 9 |
| HBond donors | 1 |
| Atoms | 64 |
References
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