From: Clinical development of phosphatidylinositol 3-kinase inhibitors for cancer treatment
IC50 (nM) | α | E545K | H1047R | β | δ | γ | mTOR | Reference |
---|---|---|---|---|---|---|---|---|
Pan-isoform PI3K inhibitors | ||||||||
XL147 | 39 | - | - | 383 | 36 | 23 | > 15,000 | [6] |
BKM120 | 52 | 99 | 58 | 166 | 116 | 262 | 2,866 | [139] |
GDC-0941 | 3 | 3 | 3 | 33 | 3 | 75 | 580 | [140] |
PX-866 | 39 | - | - | 88 | 124 | 183 | - | [13] |
BAY 80-6946 | 0.5 | - | - | 3.7 | 0.7 | 6.4 | - | [11] |
CH5132799 | 14 | 6.7 | 56 | 120 | 500 | 36 | - | [12] |
Dual pan-isoform PI3K and mTOR inhibitors | ||||||||
XL765 | 39 | - | - | 113 | 43 | 9 | 190/908 | [14] |
BEZ235 | 4 | 5.7 | 4.6 | 75 | 7 | 5 | 20.7 | |
PF-04691502* | 1.8 | - | - | 2.1 | 1.6 | 1.9 | 16 | [142] |
PF-05212384 | 0.4 | 0.6 | 0.8 | 6 | 8 | 6 | 1 | [143] |
GDC-0980 | 4.8 | - | - | 27 | 6.7 | 14 | 17 | [144] |
GSK2126458* | 0.019 | 0.0078 | 0.0094 | 0.13 | 0.024 | 0.06 | 0.18/0.3 | [18] |
BGT-226 | 4 | - | - | 63 | - | 38 | - | [24] |
PI3Kα-specific inhibitors | ||||||||
BYL719 | 5 | 4 | 5 | 1,156 | 290 | 250 | > 9,100 | [145] |
PI3Kβ-specific inhibitors | ||||||||
GSK2636771 | - | - | - | 5.2 | 58 | - | - | [86] |
PI3Kδ-specific inhibitors | ||||||||
GS-1101 (CAL-101) | 820 | - | - | 565 | 2.5 | 89 | > 1,000 | [46] |
AMG319 | - | - | - | - | < 10 | - | - | [52] |