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PI3KAD-Deg-5 | PI3KAD-Deg-5 : Degrader (PROTAC) of PIK3CA, PIK3CD
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PIK3CA
  • IC50:0.34 nM
  • DC50:0.05 nM
  • IC50:0.06 nM
  • IC50:2.65 nM
PIK3CD
  • IC50:1.85 nM
    Degrader (PROTAC)
    up to 100 nM

    Selectivity

    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    Whole-proteome analysis demonstrated that PI3Kα was significantly degraded by D5 in T47D cells, but ...
    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    >10,000-fold degradation selectivity over the PI3Kβ and PI3Kγ isoforms

    Potency
    Cellular
    In Vitro

    PIK3CA

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.5c03368

    PIK3CD

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.5c03368

    In Vivo Validations

    Rat
    Dose: 1 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 4.43 h
    Systemic clearance: 1.99 L/h/Kg
    Cmax: 4612.84 ng/mL
    Area Under the Curve:: 510.26 h*ng/mL

    DOI Reference: 10.1021/acs.jmedchem.5c03368

    Dose: 10 mg/Kg
    Route of delivery: Oral
    Plasma half life: 1.66 h
    Systemic clearance: 108.80 L/h/Kg
    Cmax: 17.30 ng/mL
    Tmax: 1.44 h
    Area Under the Curve:: 94.26 h*ng/mL
    Bioavailability: 1.85%

    DOI Reference: 10.1021/acs.jmedchem.5c03368

    Negative Control Compounds

    D5Me
    Notes: D5Me not degraded the PI3Kα protein
    SMILES: COC1=C2C(C3=NCCN3C(NC(C4=CN=C(N)N=C4)=O)=N2)=CC=C1OCCCN5CCN(CCCCCCCC(NC6=C(C(N(C7CCC(N(C)C7=O)=O)C8)=O)C8=CC=C6)=O)CC5

    Chemical Information

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    References

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    Expert Reviews

    No SERP comments found for PI3KAD-Deg-5

    Probe PI3KAD-Deg-5 is in the process of SERP review.

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