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TANZISERTIB | TANZISERTIB : Inhibitor of JNK1, JNK2, JNK3
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
MAPK8
  • IC50:61 ± 24 nM
  • Ki:44 ± 3 nM
  • IC50:1000 nM
MAPK9
  • IC50:7 ± 2 nM
  • Ki:6.2 ± 0.6 nM
    MAPK10
    • IC50:6 ± 2 nM
      Inhibitor
      up to 1 uM

      Selectivity

      In Vitro Selectivity Assessment
      Potency Assay Off-Target:
      Selective against MAP kinases ERK1 and p38α with IC50 of 0.48 and 3.4 μM respectively.
      In Vitro Selectivity Assessment
      Potency Assay Off-Target:
      Tanzisertib showed remarkable selectivity in a panel of 240 kinases, EGFR being the only non-MAP kin ...

      Potency
      Cellular
      In Vitro

      MAPK8

      Mode of Action: Inhibitor

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1016/j.bmcl.2011.12.027

      MAPK9

      Mode of Action: Inhibitor

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1016/j.bmcl.2011.12.027

      MAPK10

      Mode of Action: Inhibitor

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1016/j.bmcl.2011.12.027

      In Vivo Validations

      Rat
      Dose: 2 mg/Kg
      Route of delivery: Intravenous
      Plasma half life: 0.7 h MRT
      Systemic clearance: 39 mL/min/kg
      Area Under the Curve:: 1.9 uM*h
      Volume of Distribution at Steady-State: 1.7 L/Kg

      DOI Reference: 10.1016/j.bmcl.2011.12.027

      Dose: 10 mg/Kg
      Route of delivery: Oral
      Cmax: 7.2 uM
      Tmax: 1.5 h
      Area Under the Curve:: 86 uM*h
      Bioavailability: 30%

      DOI Reference: 10.1016/j.bmcl.2011.12.027

      Dog
      Dose: 1 mg/Kg
      Route of delivery: Intravenous
      Plasma half life: 7.3 h MRT
      Systemic clearance: 3.4 mL/min/Kg
      Area Under the Curve:: 11 uM*h
      Volume of Distribution at Steady-State: 1.5 L/Kg

      DOI Reference: 10.1016/j.bmcl.2011.12.027

      Dose: 10 mg/Kg
      Route of delivery: Oral
      Cmax: 7.2 uM
      Tmax: 2.5 h
      Area Under the Curve:: 86 uM*h
      Bioavailability: 27-93%

      DOI Reference: 10.1016/j.bmcl.2011.12.027

      Monkey (Cynomolgus)
      Dose: 1 mg/Kg
      Route of delivery: Intravenous
      Plasma half life: 10 h MRT
      Systemic clearance: 2.9 mL/min/Kg
      Area Under the Curve:: 13 uM*h
      Volume of Distribution at Steady-State: 1.6 L/Kg

      DOI Reference: 10.1016/j.bmcl.2011.12.027

      Dose: 10 mg/Kg
      Route of delivery: Oral
      Cmax: 11 uM
      Tmax: 1.3 h
      Area Under the Curve:: 100 uM*h
      Bioavailability: 77%

      DOI Reference: 10.1016/j.bmcl.2011.12.027

      Chemical Information

      Molecular Formula C21H23F3N6O2
      InChI InChI=1S/C21H23F3N6O2/c22-11-7-15(23)18(16(24)8-11)28-21-27-17-9-25-20(26-12-1-3-14(31)4-2-12)29-19(17)30(21)13-5-6-32-10-13/h7-9,12-14,31H,1-6,10H2,(H,27,28)(H,25,26,29)/t12-,13-,14-/m0/s1
      Molecular weight 448.18 Da
      AlogP 0.0
      HBond acceptors 8
      HBond donors 3
      Atoms 55

      References

      Publications

      Cross References

      canSARChEMBLBindingDBPDB

      Expert Reviews

      by SERP
      (on 21 May 2025 )
      Cellular Use Rating
      In Model Organisms
      Tanzisertib is a high-quality chemical probe for potently inhibiting JNK1, JNK2, and JNK3. It is > 20-fold selective over p38 and ERK1, although it does have modest off-target activity (IC50 ~ 400 nM)...
      Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria