AXL-IN-68 |
AXL-IN-68 : Inhibitor of AXL
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| AXL |
|
|
Inhibitor
up to 100 nM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Cpd 68 was evaluated for selectivity against a large panel of 403 mutant and nonmutant kinases to de ...
Potency Cellular
In Vitro
AXL
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/acs.jmedchem.5c00238
In Vivo Validations
Rat
Dose: 0.25 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
2.1 h
Systemic clearance:
0.14 L/h/Kg
Volume of Distribution at Steady-State:
0.34 L/Kg
DOI Reference: 10.1021/acs.jmedchem.5c00238
Dose: 2.0 mg/Kg
Route of delivery:
Oral
Cmax:
1000 ng/mL
Tmax:
2.0 h
Area Under the Curve::
4300 h*ng/mL
Bioavailability:
30%
DOI Reference: 10.1021/acs.jmedchem.5c00238
Chemical Information
| Molecular Formula | C31H33N5O2 |
| SMILEs | CN(C)C(=O)c1ccc(-c2n[nH]c3ncc(-c4ccc5c(c4)CC[C@@H](N4C6COCC4C6)CC5)cc23)cc1 |
| InChI | InChI=1S/C31H33N5O2/c1-35(2)31(37)21-6-4-20(5-7-21)29-28-14-24(16-32-30(28)34-33-29)23-8-3-19-9-11-25(12-10-22(19)13-23)36-26-15-27(36)18-38-17-26/h3-8,13-14,16,25-27H,9-12,15,17-18H2,1-2H3,(H,32,33,34)/t25-,26?,27?/m0/s1 |
| Molecular weight | 507.26 Da |
| AlogP | 4.714200000000004 |
| HBond acceptors | 7 |
| HBond donors | 1 |
| Atoms | 71 |