PI3KAD-Deg-5

PI3KAD-Deg-5 : Degrader (PROTAC) of PIK3CA, PIK3CD

Structure

SERP Rating

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Information

PIK3CA
PIK3CD

Degrader (PROTAC)

up to 100 nM

In Vitro Validations

Uniprot ID: P42336

Target Class: Kinase

Target SubClass: PI3/PI4 family

Potency: IC50

Potency Value: 0.34 nM

Potency Assay: ATP-Glo kinase viability assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Phosphatidylinositol 4,5-bisphosphate 3-kinase cat ...

DOI Reference: 10.1021/acs.jmedchem.5c03368

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay, off target (cells): Whole-proteome analysis demonstrated that PI3Kα was significantly degraded by D5 in T47D cells, but other PI3K isoforms, regulatory subunits and key proteins in the PAM pathway did not show significant degradation, such as PIK3CB, PIK3R2/4 and mTOR.

Potency assay, off target (cells): >10,000-fold degradation selectivity over the PI3Kβ and PI3Kγ isoforms

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