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Table 1 EC50 values generated for hits from primary screen

From: PI3K/AKT/mTOR inhibition in combination with doxorubicin is an effective therapy for leiomyosarcoma

Pathway Target Drug EC50 72 h (nM)
SKLMS1 STS39
PI3K/AKT/mTOR PI3K PIK-75 10.79 14.9
PIK-90 1705.3 952.2
BKM120 800.0 513.2
ZSTK474 149.0 318.8
PF-04691502* 59.3 57.0
BEZ235* 62.8 73.5
AKT A-443654 313.8 430.1
GSK-690693
MK-2206 933.5 486.9
mTOR AZD-8055 12.1 12.61
OSI-027
Everolimus -
KU0063794 434.3 240.1
Rapamycin
Cell cycle regulators G2/M Chk 1 and 2 AZD-7762 139.9 1001.0
PLK1 BI-2536 1922.0
GSK-461364 6.7
BI-6727 (volasertib)
Cell cycle regulators G1/S Wee-1 MK-1775 40.0
Other RTK LIMK LIM2K
  1. EC50 values generated by the 20 hits found in the primary screen for both STS39 and SKLMS1. The 10-point dilution curve includes doses ranging from 0.25 to 5000 nM. Highlighted boxes are inhibitors used in further studies. Inhibitors with dash (–) indicate no EC50 value was generated, * indicates a dual inhibitor targeting both PI3K and mTOR