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The compound showed poor selectivity to PI3K alpha (IC50 value of 55 ± 16 nM). A cellular target engagement assay is not available.
(last updated:
22 Mar 2023 )
SERP+
Ratings
In Cell Rating
SERP+
Comments:
The compound possesses good in vitro and in cell potency. There is however insufficient selectivity for PI3K-delta and PI3K-gamma over PI3K-alpha. Whilst IC50 values show ~20-fold difference (PI3K-alpha: 55 nM, PI3K-delta: 2.1 nM, PI3K-gamma: 6.5 nM), KINOMEscan screening shows additional significant inhibition of PI3K-alpha (<35 %control). The KINOMEscan results further reveal up to 9 other potential off-targets with strong inhibition (<35 %control). The compound is well characterised in different cell lines with extensive cytotoxicity assays and possible use up to 10 uM depending on cell type. Existing successful inhibitors such as Idelalisib and Duvelisib are already available for these targets.
