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Table 2 Isoform specificity of some of the phosphatidylinositol 3-kinase (PI3K) inhibitors in clinical development

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 [16, 141]
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]
  1. A dash indicates no data available.
  2. mTOR = mammalian target of rapamycin.
  3. Ki*: binding affinity