Table 1

PI3K-related kinase isoform selectivity of compounds used in in vitro studies

DrugSpecified targetsIC50References
PI3KmTORDNA-PKATM
BEZ235 PI3K/mTOR 4-75 nM 8 nM 1.7 nM <100 nM 23, 38, 39, 40 
BKM120 PI3K 2-262 nM 2.9 μM >10 μM N/R 46 
Everolimus mTORC1 N/A <10 nM N/A N/A 23 
KU63794 mTORC1/2 >10 μM 10 nM N/R N/R 47 
KU57788 DNA-PK 5 μM 1.7 μM 14 nM >100 nM 48 
KU55933 ATM 17 μM 9 μM 2.5 μM 13 nM 45 
DrugSpecified targetsIC50References
PI3KmTORDNA-PKATM
BEZ235 PI3K/mTOR 4-75 nM 8 nM 1.7 nM <100 nM 23, 38, 39, 40 
BKM120 PI3K 2-262 nM 2.9 μM >10 μM N/R 46 
Everolimus mTORC1 N/A <10 nM N/A N/A 23 
KU63794 mTORC1/2 >10 μM 10 nM N/R N/R 47 
KU57788 DNA-PK 5 μM 1.7 μM 14 nM >100 nM 48 
KU55933 ATM 17 μM 9 μM 2.5 μM 13 nM 45 

Kinase inhibition 50% inhibitory concentration (IC50) for each compound as reported in selected references. Targets inhibited in the nanomolar concentration range are in italics.

N/A, not applicable, N/R, not reported.

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