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ITACITINIB | ITACITINIB : Inhibitor of JAK1
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
JAK1
  • IC50:3.2 nM
  • IC50:21 ± 11nM
  • IC50:35 ± 15 nM
  • IC50:76 ± 40 nM
  • Activity:10 nM
Inhibitor
up to 100 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity within target family: Itacitinib was a selective JAK1 inhibitor with an IC50 value of 3. ...
Selectivity Assessment Description:
At a test concentration of 100 nM, itacitinib did not show significant inhibition (<30% inhibition) ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Thrombopoietin induced STAT3 phosphorylation of PBMC: 913 ± 87 nM.
Selectivity Assessment Description:
JAK2 specific thrombopoietin induced STAT3 phosphorylation required >10 fold higher itacitinib conce ...

Potency
Cellular
In Vitro

JAK1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.ejphar.2020.173505

In Vivo Validations

Mouse
Dose: 20, 40, and 80 mg/k
Route of delivery: Oral
Cmax: 1361, 1800, 7025 nM
Area Under the Curve:: 2609, 3783,10784 uM*h

DOI Reference: 10.1016/j.ejphar.2020.173505

Orthogonal Probes def

RUXOLITINIB
BARICITINIB

Chemical Information

Molecular Formula C26H23F4N9O
InChI InChI=1S/C26H23F4N9O/c27-20-18(1-7-32-22(20)26(28,29)30)24(40)37-9-3-17(4-10-37)38-13-25(14-38,5-6-31)39-12-16(11-36-39)21-19-2-8-33-23(19)35-15-34-21/h1-2,7-8,11-12,15,17H,3-5,9-10,13-14H2,(H,33,34,35)

References

Publications

Cross References

canSARChEMBLBindingDBPDB

Expert Reviews

by SERP
(on 19 May 2025 )
Cellular Use Rating
In Model Organisms
Itacitinib is a well-characterized potent inhibitor of JAK1. Due to the small (22-fold) selectivity window between JAK1 (IC50 = 3.2 nM) and JAK2 (72 nM) inhibition I recommend to include the JAK2-selective...
by SERP
(on 5 Jul 2025 )
Cellular Use Rating
In Model Organisms
Itacitinib is a potent JAK1 inhibitor (IC50=3.2 nM @ 1mM ATP) that shows efficacy across a number of JAK1 dependent cell models and in vivo models of inflammatory diseases. While being rather selective...
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