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eCF309 | eCF309 : ATP competitive inhibitor of MTOR
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
MTOR
  • IC50:15 nM
  • IC50, EC50:<30nM; 8-72 nM
ATP competitive
20-50 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - DDR1/2 2,110 nM, DNA-PK 320 nM, PI3Kα 981 nM, PI3Kβ >10,000 nM, PI3Kγ 1,340 nM, PI3Kδ 1,840 nM

Selectivity Assessment Description:
Kinome profiling of eCF309 against 375 wild type and mutant kinases was performed at 10 μM. mTOR was ...

Potency
Cellular
In Vitro

MTOR

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? No

Orthogonal Probes def

Rapamycin
AZD2014

Chemical Information

Molecular Formula C18H21N7O3
SMILEs CCOC(Cn1nc(-c2ccc3oc(N)nc3c2)c2c(N)ncnc21)OCC
InChI InChI=1S/C18H21N7O3/c1-3-26-13(27-4-2)8-25-17-14(16(19)21-9-22-17)15(24-25)10-5-6-12-11(7-10)23-18(20)28-12/h5-7,9,13H,3-4,8H2,1-2H3,(H2,20,23)(H2,19,21,22)
Molecular weight 383.17 Da
AlogP 2.1980000000000004
HBond acceptors 10
HBond donors 4
Atoms 49

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Expert Reviews

by SERP
(on 21 Dec 2016)
Cellular Use Rating
eCF309 appears sufficiently potent in cell-free systems (15 nM). Strong evidence is provided with regards to kinase selectivity in biochemical assays. Solid kinase profiling was performed in the original...
by SERP
(on 20 Jan 2017)
Cellular Use Rating
eCF309 is a potent inhibitor of mTOR signaling. The compound is potent in a target-based assay and in cellular systems. eCF309 has been profiled against 375 wild-type and mutant kinases and has an S(35)...
by SERP
(on 17 Mar 2017)
Cellular Use Rating
eCF309 has been thoroughly profiled against other kinases and moderate activity was detected for only a few of them. Potential in vitro affinities against targets that are phylogenetically more distantly...
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