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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

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