Chemical Probes logo
AZD2014 | AZD2014 : ATP competitive inhibitor of MTOR
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

More...

Targets Biochemical/Biophysical Potency Cellular Potency
MTOR
  • IC50:2.8 nM
  • IC50:80 nM
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

Orthogonal Probes def

Rapamycin
eCF309

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

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 27 May 2016)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
by SERP
(on 1 Jun 2016)
Cellular Use Rating
In Model Organisms
Selectivity over 200 typical protein kinases and PI3Ks is >1000X. However, selectivity over atypical lipid-like protein kinases (e.g., ATM, ATR, DNA-PK) does not appear to have been disclosed, and this...
by SERP
(on 5 Jan 2017)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria