Table 1

Kinase inhibition profile of CAL-101

IC50 (nM)Fold-selectivity, PI3K
Class IClass IIClass IIIClass IVOthers
p110δ p110α p110β p110γ CIIβ hVPS34 DNA-PK mTOR PIP5Ka PIP5Kb 
2.5 > 300× > 200× > 40× > 400× > 400× > 3000 × > 4000 × > 400 × > 400 × 
IC50 (nM)Fold-selectivity, PI3K
Class IClass IIClass IIIClass IVOthers
p110δ p110α p110β p110γ CIIβ hVPS34 DNA-PK mTOR PIP5Ka PIP5Kb 
2.5 > 300× > 200× > 40× > 400× > 400× > 3000 × > 4000 × > 400 × > 400 × 

CAL-101 shows PI3K/p110δ selectivity in kinase profiling assay.

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