INCB127443 |
INCB127443 : Inhibitor of CDK2
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| CDK2 |
|
|
up to 100 nM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity within target family: IC50s
CDK1/B1 (nM) 313 (316×); CDK4/D1 (nM) 12 (12×); CDK5/p35 (nM ...
Selectivity Assessment Description:
In Cell Selectivity Assessment
Potency Assay Off-Target:
Selectivity whithin target family IC50s assessed in cells:
CDK1 OVCAR-3 pNPM (nM) 518 (25×); CDK4 Je ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
General kinome selectivity, INCB127443 was profiled against an in-house panel of 37 kinases and exhi ...
Selectivity Assessment Description:
Off-target activity observed outside the CDK family was primarily associated with CMGC kinases (DYRK ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
NanoBRET selectivity: CDK1/cyclin B1 (IC50 = 176 nM), CDK4/cyclin D1 (IC50 = 37 nM), and CDK6/cyclin ...
Potency Cellular
In Vitro
CDK2
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/acs.jmedchem.6c01506
In Vivo Validations
Rat
Dose: 3 mg/Kg
Route of delivery:
Oral
Cmax:
823 nM
Area Under the Curve::
3518 nM·h
Bioavailability:
94%
DOI Reference: 10.1021/acs.jmedchem.6c01506
Dose: 0.5 nM
Route of delivery:
Intravenous
Plasma half life:
4.8 h
Volume of Distribution at Steady-State:
4.7 L/Kg
DOI Reference: 10.1021/acs.jmedchem.6c01506
Monkey (Cynomolgus)
Dose: 1 mg/Kg
Route of delivery:
Oral
Cmax:
435 nM
Area Under the Curve::
4695 nM·h
Bioavailability:
64%
DOI Reference: 10.1021/acs.jmedchem.6c01506
Dose: 0.3 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
10 h
Volume of Distribution at Steady-State:
2.3 L/Kg
DOI Reference: 10.1021/acs.jmedchem.6c01506
Chemical Information
| SMILES | CS(=O)(=O)N1CCC(CC1)Nc2ncc(c(n2)c3cn(cn3)c4ccc(CN5CCC5)c(F)c4Cl)C(F)(F)F |