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2-MT 63 | Inhibitor of TEK
RATINGS:
Cellular Use: (3 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
TEK
  • IC50:30 nM
  • IC50:62 nM
Inhibitor
10-1,000 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - VEGFR: 7,800 nM, IGFR1: 927 nM

Potency Assay Off-Target:
In HTRF assays (as above) on 28 kinases, the compound was at least 30-fold selective for TIE2. Kinas ...
Selectivity Assessment Description:
Not done.

Potency
Cellular
In Vitro

TEK

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

In Vivo Validations

Sprague-Dawley male rat
Dose: 1 mg/kg (IV), 10 mg/kg (oral)
Route of delivery: Intravenous, Oral
Plasma half life: 1.6 h
Systemic clearance: 1,300 mL/h/kg
Organ of interest (O): mouse lung
Target engagement assay: Indirect, inhibition of Ang-1-induced Tie2 autophosphorylation assayed by western blot

Reference: --

Orthogonal Probes def

BAY-826

Chemical Information

Molecular Formula C29H30F4N8O2
SMILEs CNc1ncnc(-c2cccnc2Oc2ccc(F)c(C(=O)Nc3cc(C(F)(F)F)ccc3N(C)CCCN(C)C)c2)n1
InChI InChI=1S/C29H30F4N8O2/c1-34-28-37-17-36-25(39-28)20-7-5-12-35-27(20)43-19-9-10-22(30)21(16-19)26(42)38-23-15-18(29(31,32)33)8-11-24(23)41(4)14-6-13-40(2)3/h5,7-12,15-17H,6,13-14H2,1-4H3,(H,38,42)(H,34,36,37,39)
Molecular weight 598.24 Da
AlogP 5.5657
HBond acceptors 10
HBond donors 2
Atoms 73

References

Publications

    Cross References

    canSARChEMBLBindingDB

    Expert Reviews

    by SERP
    (on 17 Mar 2017 )
    Cellular Use Rating
    In Model Organisms
    2-MT 63 represents a novel inhibitor of the TIE2 receptor. There are multiple kinase inhibitors that have validated activity versus the TIE2 receptor including the advanced clinical agents, Sitravatinib,...
    by SERP
    (on 29 Mar 2017 )
    Cellular Use Rating
    In Model Organisms
    2-MT 63 is a novel TIE-2 kinase inhibitor that demonstrates unique and improved kinase selectivity compared to other inhibitors known to interact with TIE-2. The developmental focus centered on in vivo...
    by SERP
    (on 15 May 2017 )
    Cellular Use Rating
    In Model Organisms
    2-MT 63 has a good kinase selectivity profile in enzyme assays with >30-fold selectivity (typically much greater) against the tested kinases. Importantly, the profile includes selectivity against other...
    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