AZD-6482
AZD-6482 : ATP competitive inhibitor of PIK3CB
Structure
In Cells
In Model Organisms
SERP ratings and comments
SERP Ratings
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
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
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 )