YYSW001 |
YYSW001 : Inhibitor of JAK1
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download
Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| JAK1 |
|
|
Inhibitor
up to 1 uM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
KinomeSCAN Screening at concentration of 1000 nM, against a panel of 403 kinases demonstrated remark ...
Selectivity Assessment Description:
YYSW001 potently inhibited only two kinases, which were the intended target JAK1 and the only off-ta ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
GM-CSF-induced STAT5 phosphorylation (JAK2-STAT5 IC50 = 5.530 μM).
Potency Cellular
In Vitro
JAK1
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/acs.jmedchem.5c03183
In Vivo Validations
Rat
Dose: 3 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
2.8 ± 0.3 h
Systemic clearance:
0.7 ± 0.1 L/h/Kg
Area Under the Curve::
3831.25 ± 547.5 h·μg/L
Volume of Distribution at Steady-State:
3.1 ± 0.4 L/Kg
DOI Reference: 10.1021/acs.jmedchem.5c03183
Dose: 3 mg/Kg
Route of delivery:
Oral
Plasma half life:
2.8 ± 0.2 h
Systemic clearance:
1.2 ± 0.2 L/h/Kg
Cmax:
328.61 ± 86.7 μg/L
Tmax:
3.0 ± 1.1 h
Area Under the Curve::
2277.65 ± 438.1 h·μg/L
Bioavailability:
61.8%
Volume of Distribution at Steady-State:
5.0 ± 1.0 L/Kg
DOI Reference: 10.1021/acs.jmedchem.5c03183
Dose: 5 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
1.96 ± 0.33 h
Systemic clearance:
2.41 ± 0.13 L/h/Kg
Area Under the Curve::
2054.79 ± 110.71 h·μg/L
Volume of Distribution at Steady-State:
6.78 ± 1.05 L/Kg
DOI Reference: 10.1021/acs.jmedchem.5c03183
Dose: 10 mg/Kg
Route of delivery:
Oral
Plasma half life:
2.2 ± 0.6 h
Systemic clearance:
1.1 ± 0.1 L/h/kg
Cmax:
1323.53 ± 328.2 μg/L
Tmax:
3.2 ± 1.3 h
Area Under the Curve::
8543.24 ± 971.2 h·μg/L
Bioavailability:
65.6%
Volume of Distribution at Steady-State:
3.6 ± 1.3 L/Kg
DOI Reference: 10.1021/acs.jmedchem.5c03183
Chemical Information
Coming Soon...