PF-07265028 |
PF-07265028 : Inhibitor of MAP4K1
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download
Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| MAP4K1 |
|
|
Inhibitor
up to 100 nM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
kinome selectivity was assessed using an Invitrogen 21-kinase mini-panel showed very high selectivit ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
PF-07265028 was further profiled in the full Invitrogen panel (395 kinases, 402 assays, with follow ...
Selectivity Assessment Description:
2 out of 395 kinases (MAP4K5 and TAOK1) have the potential to be inhibited at a less than 30-fold wi ...
Potency Cellular
In Vitro
MAP4K1
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/acs.jmedchem.4c01930
In Vivo Validations
Mouse
Dose: 1 mg/kg IV, 15 mg/kg PO
Route of delivery:
Intravenous, Oral
Plasma half life:
3.3 ± 0.3 h
Systemic clearance:
39 ± 0.6 mL/min/mg
Tmax:
2.0 ± 1.7 h
Bioavailability:
38% PO
Volume of Distribution at Steady-State:
4.9 ± 0.7 L/Kg
DOI Reference: 10.1021/acs.jmedchem.4c01930
Monkey (Cynomolgus)
Dose: 0.5 mg/kg IV, 1 mg/kg PO
Route of delivery:
Intravenous, Oral
Plasma half life:
4.3 h
Systemic clearance:
14 mL/min/mg
Tmax:
1.0 h
Bioavailability:
20% PO
Volume of Distribution at Steady-State:
3.7 L/Kg
DOI Reference: 10.1021/acs.jmedchem.4c01930
Chemical Information
| Molecular Formula | C26H32N8O |
| SMILEs | CC[C@H](N)c1nc(N2CCC[C@H]2C)cc2c1CN(c1cccc(-c3nnc4n3[C@@H](C)CC4)n1)C2=O |
| InChI | InChI=1S/C26H32N8O/c1-4-19(27)24-18-14-33(26(35)17(18)13-23(29-24)32-12-6-7-15(32)2)21-9-5-8-20(28-21)25-31-30-22-11-10-16(3)34(22)25/h5,8-9,13,15-16,19H,4,6-7,10-12,14,27H2,1-3H3/t15-,16+,19+/m1/s1 |
| Molecular weight | 472.27 Da |
| AlogP | 0.0 |
| HBond acceptors | 9 |
| HBond donors | 2 |
| Atoms | 67 |