AZ9567 |
AZ9567 : Inhibitor of MAT2A
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 |
|---|---|---|
| MAT2A |
|
|
up to 1 uM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
The selectivity of AZ'9567 was investigated to assess its suitability as a quality in vivo tool with ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
AZ'9567 was also characterized in a broad suite of in vitro cell-based assays representing hepatic, ...
Potency Cellular
In Vitro
MAT2A
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/acs.jmedchem.3c01860
In Vivo Validations
Mouse
Dose: 0.5 mg/Kg
Route of delivery:
Intravenous
Area Under the Curve::
1.38 uM*h
DOI Reference: 10.1021/acs.jmedchem.3c01860
Dose: 1 mg/Kg
Route of delivery:
Oral
Cmax:
0.29 uM
Tmax:
4.0 h
Area Under the Curve::
2.98 uM*h
Bioavailability:
108%
DOI Reference: 10.1021/acs.jmedchem.3c01860
Rat
Dose: 0.5 mg/Kg
Route of delivery:
Intravenous
Area Under the Curve::
11.0 uM*h
DOI Reference: 10.1021/acs.jmedchem.3c01860
Dose: 1 mg/Kg
Route of delivery:
Oral
Cmax:
2.44 uM
Tmax:
2.0 h
Area Under the Curve::
27.8 uM*h
Bioavailability:
127%
DOI Reference: 10.1021/acs.jmedchem.3c01860
Chemical Information
| Molecular Formula | C24H19F2N5O2 |
| SMILEs | Cn1cc2cc(-c3cc4n[nH]c(C5CC5)c4n(-c4ccc(OC(F)F)cc4)c3=O)ccc2n1 |
| InChI | InChI=1S/C24H19F2N5O2/c1-30-12-15-10-14(4-9-19(15)29-30)18-11-20-22(21(28-27-20)13-2-3-13)31(23(18)32)16-5-7-17(8-6-16)33-24(25)26/h4-13,24H,2-3H2,1H3,(H,27,28) |
| Molecular weight | 447.15 Da |
| AlogP | 4.746300000000003 |
| HBond acceptors | 7 |
| HBond donors | 1 |
| Atoms | 52 |