Skip to main content

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