AZENOSERTIB |
AZENOSERTIB : Inhibitor of WEE1
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 |
|---|---|---|
| WEE1 |
|
|
Inhibitor
up to 1 uM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Azenosertib showed excellent kinase selectivity. When screened against a full panel of 476 kinases a ...
Potency Cellular
In Vitro
WEE1
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? No
DOI Reference: 10.1021/acs.jmedchem.1c01121
In Vivo Validations
Dog
Dose: 3 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
1.4 h
Systemic clearance:
46 mL/min/kg
Area Under the Curve::
2.1 μM·h
Volume of Distribution at Steady-State:
4.4 L/Kg
DOI Reference: 10.1021/acs.jmedchem.1c01121
Dose: 10 mg/Kg
Route of delivery:
Oral
Plasma half life:
2.3 h
Cmax:
2.1 μM
Area Under the Curve::
9.7 μM·h
Bioavailability:
142%
DOI Reference: 10.1021/acs.jmedchem.1c01121
Chemical Information
| Molecular Formula | C29H34N8O2 |
| SMILEs | C=CCn1c(=O)c2cnc(Nc3ccc(N4CCN(C)CC4)cc3)nc2n1-c1ccc2c(n1)[C@@](O)(CC)CC2 |
| InChI | InChI=1S/C29H34N8O2/c1-4-14-36-27(38)23-19-30-28(31-21-7-9-22(10-8-21)35-17-15-34(3)16-18-35)33-26(23)37(36)24-11-6-20-12-13-29(39,5-2)25(20)32-24/h4,6-11,19,39H,1,5,12-18H2,2-3H3,(H,30,31,33)/t29-/m1/s1 |
| Molecular weight | 526.28 Da |
| AlogP | 3.2024000000000017 |
| HBond acceptors | 10 |
| HBond donors | 2 |
| Atoms | 73 |
| PAINS * | Yes |
* This is an automated alert only, and may not necessarily indicate an issue with this probe. ( Learn more about PAINS )