FGFR3-IN-10s |
FGFR3-IN-10s : Covalent Inhibitor of FGFR3
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| FGFR3 (Mutant:WT, V555M) |
|
|
Covalent Inhibitor
up to 500 nM
Selectivity
In Cell Selectivity Assessment
Potency Assay Off-Target:
Compound 10s displayed promising FGFR3 selectivity in the cellular assays with an RT112/84 IC50 valu ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Compound 10s demonstrated improved selectivity over FGFR1/2 (43.5/5.3-fold)
In Vitro Selectivity Assessment
TNK1
Gene ID: Q13470
Organism: Homo sapiens
Family: Tyr protein kinase family
Potency: IC50 - 16.9 nM
Potency Assay Off-Target:
Kinase profiling of cpd 10s at a concentration of 0.5 μM was conducted against a panel of 330 wild-t ...
Selectivity Assessment Description:
Results demonstrated that cpd 10s displayed extraordinary kinome selectivity with S(1) and S(10) sel ...
Potency Cellular
In Vitro
FGFR3
(Mutant:WT, V555M)
Mode of Action: Covalent Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/acs.jmedchem.5c02552
In Vivo Validations
Rat
Dose: 2 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
0.47 h
Systemic clearance:
133.4 mL/min/Kg
Cmax:
656 ng/mL
Tmax:
0.083 h
Area Under the Curve::
249 h*ng/mL
DOI Reference: 10.1021/acs.jmedchem.5c02552
Dose: 10 mg/Kg
Route of delivery:
Oral
Plasma half life:
0.59 h
Cmax:
69.3 ng/mL
Tmax:
0.25 h
Area Under the Curve::
46.6 h*ng/mL
Bioavailability:
3.74%
DOI Reference: 10.1021/acs.jmedchem.5c02552
Chemical Information
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