PLK1-COV-B9 |
PLK1-COV-B9 : Covalent Inhibitor of PLK1
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| PLK1 |
|
|
Covalent Inhibitor
up to 100 nM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity within target family: selective over PLK2 and PLK3 IC50s 152 and 175 nM respectively.
In Vitro Selectivity Assessment
Potency Assay Off-Target:
PLK1-COV-B9 was screened against a panel of 435 kinases at a concentration of 10 μM.
Selectivity Assessment Description:
B9 exhibited a favorable selectivity profile at this high screening concentration. While B9 effectiv ...
Potency Cellular
In Vitro
PLK1
Mode of Action: Covalent Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/acs.jmedchem.6c01512
In Vivo Validations
Mouse
Dose: 1 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
0.512 ± 0.017 h
Systemic clearance:
51.4 ± 4.45 mL/min/Kg
Cmax:
527 ± 36.1 ng/mL
Tmax:
0.083 h
Area Under the Curve::
324 ± 29.2 h x ng/mL
Volume of Distribution at Steady-State:
1.73 ± 0.133 L/Kg
DOI Reference: 10.1021/acs.jmedchem.6c01512
Dose: 10 mg/Kg
Route of delivery:
Oral
Plasma half life:
0.879 ± 0.072 h
Cmax:
2200 ± 688 ng/mL
Tmax:
0.33 h
Area Under the Curve::
2510 ± 209 h x ng/mL
Bioavailability:
77.6 ± 6.43%
DOI Reference: 10.1021/acs.jmedchem.6c01512
Chemical Information
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