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CAPIVASERTIB | CAPIVASERTIB : Inhibitor of AKT1, AKT2, AKT3
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

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Targets Biochemical/Biophysical Potency Cellular Potency
AKT1
  • IC50:3 nM
  • IC50:89 nM
AKT2
  • IC50:8 nM
    AKT3
    • IC50:8 nM
      Inhibitor
      up to 1 uM

      Selectivity

      In Vitro Selectivity Assessment
      Potency Assay Off-Target:
      AZD5363 was assayed against a larger enzyme panel of 75 kinases, of which 35 were also AGC family ki ...
      In Cell Selectivity Assessment
      Potency Assay Off-Target:
      The cellular IC50 against P70S6K was approximately 5 μM, as measured by inhibition of S6 phosphoryla ...

      Potency
      Cellular
      In Vitro

      AKT1

      Mode of Action: Inhibitor

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1021/jm301762v

      AKT2

      Mode of Action: Inhibitor

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1021/jm301762v

      AKT3

      Mode of Action: Inhibitor

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1021/jm301762v

      In Vivo Validations

      Mouse
      Dose:
      Route of delivery: Intravenous, Oral
      Plasma half life: 0.2 h
      Systemic clearance: 207 mL/min/Kg
      Bioavailability: 86%
      Volume of Distribution at Steady-State: 4.1 L/Kg

      DOI Reference: 10.1021/jm301762v

      Rat
      Dose:
      Route of delivery: Intravenous, Oral
      Plasma half life: 0.5 h
      Systemic clearance: 95 mL/min/Kg
      Bioavailability: 13%
      Volume of Distribution at Steady-State: 4.0 L/Kg

      DOI Reference: 10.1021/jm301762v

      Dog
      Dose:
      Route of delivery: Intravenous, Oral
      Plasma half life: 1.7 h
      Systemic clearance: 22 mL/min/Kg
      Bioavailability: 37%
      Volume of Distribution at Steady-State: 2.1 L/Kg

      DOI Reference: 10.1021/jm301762v

      Orthogonal Probes def

      BAY-1125976
      Borussertib

      Chemical Information

      Molecular Formula C21H25ClN6O2
      SMILEs NC1(C(=O)N[C@@H](CCO)c2ccc(Cl)cc2)CCN(c2ncnc3[nH]ccc23)CC1
      InChI InChI=1S/C21H25ClN6O2/c22-15-3-1-14(2-4-15)17(6-12-29)27-20(30)21(23)7-10-28(11-8-21)19-16-5-9-24-18(16)25-13-26-19/h1-5,9,13,17,29H,6-8,10-12,23H2,(H,27,30)(H,24,25,26)/t17-/m0/s1
      Molecular weight 428.17 Da
      AlogP 2.1489000000000003
      HBond acceptors 8
      HBond donors 5
      Atoms 55

      References

      Publications

      Cross References

      canSARChEMBLBindingDBPDB

      Vendors

      Note: This is not an exhaustive list and does not indicate endorsement by the portal.

      Expert Reviews

      by SERP
      (on 1 Dec 2023)
      Cellular Use Rating
      In Model Organisms
      The half-life is too short and the selectivity too poor to interrogate AKT1-3 in vivo with confidence.
      by SERP+
      (on 23 Sept 2024)
      Cellular Use Rating
      In Model Organisms
      The compound is well characterized regarding on target data. However, better compounds for AKT exist (allosteric AKT inhibitors). AZD5363 offers a good alternative to allosteric AKT inhibitors, but does...
      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