APITOLISIB

APITOLISIB : Inhibitor of PIK3CA, PIK3CB, PIK3CG, PIK3CD, MTOR

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe APITOLISIB is in the process of SERP review.

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Information

PIK3CA
PIK3CB
PIK3CG
PIK3CD
MTOR

Inhibitor

up to 1 uM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: P42336

Target Class: Kinase

Target SubClass: PI3/PI4

Potency: IC50

Potency Value: 4.8 nM

Potency Assay: fluorescence polarization assay

PDB ID for probe-target interaction (3D structure): 3TL5

Target aliases:

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

DOI Reference: 10.1021/jm2009327

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Invitrogen’s SelectScreen: of the 240 total kinases in the SelectScreen panel, only 5 kinases other than the PI3K isoforms and mTOR consistently displayed greater than 60% inhibition when treated with 1 μM of Apitolisib: Fgr, Mlk1, PAK4, Syk, and Yes1. IC50s for Fgr, Mlk1, and Syk were 697, 232, and 134 nM, respectively. remarkably selective for several other members of the closely related PIKK family kinases: C2alpha IC50 = 1300 nM; C2beta IC50 = 7 94 nM; VPS34 IC50 = 2000 nM; PI4Kalpha >10 μM; PI4Kbeta >10 μM; DNA-PK Kiapp = 623 nM.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 19 Jun 2023 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 26 Jun 2023 )