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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

References

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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...
    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