Table 2.

The 25 PI3K pathway inhibitors used in this study and their profiles and structures (15–18)

PI3K inhibitors
ZSTK474 (4.8 × 10−7 mol/L)Wortmannin (9.7 × 10−6 mol/L)LY294002 (8.1 × 10−6 mol/L)
Selective PI3K inhibitorPI3K/mTOR/MLCK inhibitorPI3K/mTOR/CK2 inhibitor
PreclinicalPreclinicalPreclinical
PI103 (1.8 × 10−7 mol/L)PX866 (1.4 × 10−6 mol/L)NVP-BEZ235 (8.6 × 10−9 mol/L)
PI3K/mTOR inhibitorPI3Kα/δ/γ inhibitor; derivative of wortmanninPI3K/mTOR inhibitor
PreclinicalPhase IPhase I/II
GDC-0941 (5.0 × 10−7 mol/L)PI3Kα inhibitor IV (1.0 × 10−6 mol/L)TGX221 (1.0 × 10−5 mol/L)
Selective PI3K inhibitorPI3Kα/β inhibitor; derivative of PI103Selective PI3Kβ inhibitor
Phase IPreclinicalPreclinical
IC87114 (CAL-101; 8.3 × 10−5 mol/L)AS605240 (PI3Kγ inhibitor; 9.5 × 10−6 mol/L)
Selective PI3Kδ inhibitorSelective PI3Kγ inhibitor
Phase IPreclinical
Akt inhibitors
Deguelin (7.6 × 10−6 mol/L)Perifosine (9.1 × 10−6 mol/L)Akt inhibitor (1.3 × 10−5 mol/L)
Selective Akt inhibitor; derivative of rotenoneLipid-based PI analogueLipid-based PI analogue
PreclinicalPhase IIPreclinical
Akt inhibitor II (8.6 × 10−6 mol/L)Akt inhibitor III (1.9 × 10−5 mol/L)Akt inhibitor IV (2.8 × 10−7 mol/L)
Lipid-based PI analogueLipid-based PI analoguePreclinical
PreclinicalPreclinical
Akt inhibitor V (triciribine/VQD-002; 2.2 × 10−5 mol/L)Akt inhibitor VIII (AKTi-1/2; 8.6 × 10−6 mol/L)Akt inhibitor IX (8.0 × 10−7 mol/L)
Tricyclic nucleotideAllosteric Akt1/2 inhibitorPreclinical
Phase I/II (as triciribine phosphate)Preclinical
Akt inhibitor X (3.6 × 10−6 mol/L)Akt inhibitor XI (1.1 × 10−5 mol/L)
PreclinicalPreclinical
mTOR inhibitors
Rapamycin (1.7 × 10−7 mol/L)Everolimus (RAD001; 3.6 × 10−8 mol/L)Temsirolimus (CCI779; 2.0 × 10−7 mol/L)
Allosteric inhibitor of mTORC1RapalogueRapalogue
In clinical useIn clinical useIn clinical use

NOTE: Numbers in parentheses are mean GI50 values across the JFCR39 cell lines.