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Table 1 IC50s of endometrial cancer cell lines (n = 13) to the PI3Ki pictilisib, PI3K/mTORi apitolisib and the MEKi cobimetinib as single agents (n = 13), and the combination of pictilisib with cobimetinib and apitolisib with cobimetinib (n = 11)

From: Preclinical evaluation and reverse phase protein Array-based profiling of PI3K and MEK inhibitors in endometrial carcinoma in vitro

Cell Line Mutational status PTEN expression PI3Ki Pictilisib (uM) PI3K/mTORi
Apitolisib (uM)
MEKi
Cobimetinib (uM)
Combination of Pictilisib:Cobimetinib (uM) Combination of Apitolisib:Cobimetinib (uM)
IC50 IC50 IC50 IC50 CI at ED75 IC50 CI at ED75
SKUT2 PIK3CA only High 0.413 0.196 0.101 0.096 0.138 0.049 0.152
MFE280 PIK3CA only High 0.440 0.247 0.461 0.207 0.357 0.091 0.528
EN1078D PTEN + PIK3R1 High 0.242 0.079 0.178 0.103 0.634 0.057 0.468
MFE296 PTEN + PIK3CA High 0.273 0.106 0.301 0.383 1.037 0.120 0.650
ETN1 PTEN High 0.544 0.387 1.077 0.174 0.426 0.177 0.495
AN3CA PTEN + PIK3R1 Low 0.057 0.028 0.518 0.339 0.129 0.070 0.142
HEC59 PTEN + PIK3R1 Low 0.189 0.018 3.289
EN PTEN + PIK3CA + PIK3R1 Low 1.597 0.548 36.511 3.117 1.555 2.175 1.200
HEC1A KRAS + PIK3CA High 2.054 0.214 0.012
HEC1B KRAS + PIK3CA High 0.798 0.704 0.033 0.050 0.031 0.054 0.035
HEC50 KRAS + PIK3R1 High 0.247 0.210 0.001 0.131 4.921 0.169 6.613
EFE184 WT for all High 0.372 0.368 0.149 0.074 0.433 0.157 0.328
KLE WT for all High 2.796 7.253 39.337 0.644 0.142 0.144 0.005
  1. Drug combinations exhibiting antagonistic effects (CI values > 1) are in shown bold
  2. IC50 inhibitor concentration to inhibit 50% of the cell growth, PI3Ki PI3K inhibitor, PI3K/mTORi PI3K/mTOR inhibitor, MEKi MEK inhibitor, CI Combination Index, ED75 Effective Dose exhibiting 75% of loss in cell viability
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