AZD-6482

Inhibitor, ATP competitive of PIK3CB

Structure

Information

Protein target names: PIK3CB

Mechanism of action: Inhibitor, ATP competitive

In Vitro Validations

Uniprot ID: P42338
Target Class: Lipid kinase
Target SubClass: Class I
Potency: IC50
Potency Value: 0.69 nM
Potency Assay: In Vitro kinase assay measurements against recombinant PI3Ks and PIKK using SelectScreen (Invitrogen)
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Phosphatidylinositol 4,5-bisphosphate 3-kinase cat ...

In Cell Validations

In Vivo Data

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

Given that the profiling data available at this point uses an in vitro affinity binding assay that does not use ATP, it is difficult to assess the intracellular selectivity profile (which may very well be even better). That said, the probe appears to have decent selectivity within and outside the PI3K family. The fact that the probe appears to be selectively active against tumours driven by PTEN loss, only when they do not also have a p110 alpha activating mutation, adds to the promise and utility of this probe. Highest utility is likely to be in systems with low expression of, and biological process dependence on, the delta and gamma isoforms.

(last updated: 23 Nov 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

AZ6482 is a highly selective and potent chemical probe for PI3Kbeta. It is suitable for study the role of the target in model cell systems and animal studies.

(last updated: 8 Dec 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

AZD-6482 is a suitable chemical probe for assessing PIK3CB (PI3Kbeta) function. The compound is 8-fold selective over PI3Kdelta in in vitro assays and so care should be taken when used in cellular studies to differentiate PI3Kbeta from PI3Kdelta activity in certain contexts.

(last updated: 18 Dec 2020 )