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APITOLISIB | APITOLISIB : Inhibitor of PIK3CA, PIK3CB, PIK3CG, PIK3CD, MTOR
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
PIK3CA
  • IC50:4.8 nM
  • IC50:307 nM
  • IC50:255 nM
PIK3CB
  • IC50:27 nM
    PIK3CG
    • IC50:14 nM
      PIK3CD
      • IC50:6.7 nM
        MTOR
        • Ki:17 nM
          Inhibitor
          up to 1 uM

          Selectivity

          In Vitro Selectivity Assessment
          Potency Assay Off-Target:
          Invitrogen’s SelectScreen: of the 240 total kinases in the SelectScreen panel, only 5 kinases other ...

          Potency
          Cellular
          In Vitro

          PIK3CA

          Mode of Action: Inhibitor

          Structure-Activity-Relationship data available? Yes

          DOI Reference: 10.1021/jm2009327

          PIK3CB

          Mode of Action: Inhibitor

          Structure-Activity-Relationship data available? Yes

          DOI Reference: 10.1021/jm2009327

          PIK3CG

          Mode of Action: Inhibitor

          Structure-Activity-Relationship data available? Yes

          DOI Reference: 10.1021/jm2009327

          PIK3CD

          Mode of Action: Inhibitor

          Structure-Activity-Relationship data available? Yes

          DOI Reference: 10.1021/jm2009327

          MTOR

          Mode of Action: Inhibitor

          Structure-Activity-Relationship data available? Yes

          DOI Reference: 10.1021/jm2009327

          In Vivo Validations

          Mouse
          Dose: 1 mg/Kg
          Route of delivery: Intravenous
          Systemic clearance: 9.2 mL/min/Kg
          Volume of Distribution at Steady-State: 1.7 L/Kg

          DOI Reference: 10.1021/jm2009327

          Dose: 5 mg/Kg
          Route of delivery: Oral
          Cmax: 2.0 uM
          Area Under the Curve:: 10 uM*h
          Fb : 71%
          Bioavailability: 56%

          DOI Reference: 10.1021/jm2009327

          Dose: 50 mg/Kg
          Route of delivery: Oral
          Cmax: 24 uM
          Area Under the Curve:: 121 uM*h
          Bioavailability: 66%

          DOI Reference: 10.1021/jm2009327

          Orthogonal Probes def

          BYL719
          LENIOLISIB
          AZD2014

          Chemical Information

          Molecular Formula C23H30N8O3S
          SMILEs Cc1c(CN2CCN(C(=O)[C@H](C)O)CC2)sc2c(N3CCOCC3)nc(-c3cnc(N)nc3)nc12
          InChI InChI=1S/C23H30N8O3S/c1-14-17(13-29-3-5-31(6-4-29)22(33)15(2)32)35-19-18(14)27-20(16-11-25-23(24)26-12-16)28-21(19)30-7-9-34-10-8-30/h11-12,15,32H,3-10,13H2,1-2H3,(H2,24,25,26)/t15-/m0/s1
          Molecular weight 498.22 Da
          AlogP 0.0
          HBond acceptors 11
          HBond donors 3
          Atoms 65

          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 19 Jun 2023)
          Cellular Use Rating
          In Model Organisms
          (The reviewer did not leave any public comments)
          by SERP
          (on 26 Jun 2023)
          Cellular Use Rating
          In Model Organisms
          (The reviewer did not leave any public comments)
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