AZD-7648 |
AZD-7648 : Inhibitor of PRKDC
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary
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| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| PRKDC |
|
|
Inhibitor
up to 500 nM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Panel of 397 Kinases at Thermofisher
Selectivity Assessment Description:
Within target family - Only PI3 kinases had >50% inhibition at 1 μM. TR-FRET IC50 results: PI3Kγ 52 ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
Cell Selectivity versus Structurally Related PIKKs and PI3 Kinases: PI3Kγ (RAW-264, pAKT Thr308) IC ...
Potency Cellular
In Vitro
PRKDC
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? No
DOI Reference: 10.1021/acs.jmedchem.9b01684
In Vivo Validations
Rat
Dose: 2 mg/Kg
Route of delivery:
Intravenous
Systemic clearance:
29 mL/min/kg
Fb :
35%
Volume of Distribution at Steady-State:
1.4 L/Kg
DOI Reference: 10.1021/acs.jmedchem.9b01684
Dose: 5 mg/Kg
Route of delivery:
Oral
Bioavailability:
105%
DOI Reference: 10.1021/acs.jmedchem.9b01684
Dog
Dose: 1 mg/Kg
Route of delivery:
Intravenous
Systemic clearance:
4.0 mL/min/kg
Fb :
21%
Volume of Distribution at Steady-State:
0.7 L/Kg
DOI Reference: 10.1021/acs.jmedchem.9b01684
Dose: 2 mg/Kg
Route of delivery:
Oral
Bioavailability:
93%
DOI Reference: 10.1021/acs.jmedchem.9b01684
Chemical Information
| Molecular Formula | C18H20N8O2 |
| SMILEs | Cc1cc2ncnn2cc1Nc1ncc2c(n1)n(C1CCOCC1)c(=O)n2C |
| InChI | InChI=1S/C18H20N8O2/c1-11-7-15-20-10-21-25(15)9-13(11)22-17-19-8-14-16(23-17)26(18(27)24(14)2)12-3-5-28-6-4-12/h7-10,12H,3-6H2,1-2H3,(H,19,22,23) |
| Molecular weight | 380.17 Da |
| AlogP | 1.5762199999999995 |
| HBond acceptors | 10 |
| HBond donors | 1 |
| Atoms | 48 |
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