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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
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

DOI Reference: 10.1021/jm061107l

In Vivo Validations

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
Cmax: 520 ng/mL
Area Under the Curve:: 2640 ng h/mL
Bioavailability: 31%
Volume of Distribution at Steady-State:  2560 mL/kg
Organ of interest (O): mouse lung
Target engagement assay: Indirect, inhibition of Ang-1-induced Tie2 autophosphorylation assayed by western blot

DOI Reference: 10.1021/jm061107l

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 5.565700000000005
HBond acceptors 10
HBond donors 2
Atoms 73

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...
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