Table 1.

IC50 values of AZD5363 against enzyme and cellular endpoints

Enzyme inhibition n mol/L
Akt13
Akt27
Akt37
ROCK1470
ROCK260
PKA7
P70S6K6
Inhibition of AKT substrates in cells μ mol/L
pGSK3β0.76 (BT474c; Western)
0.06 (LNCaP; Western)
0.38 (MDA-MB-468; Acumen)
pPRAS400.31 (BT474c; Western)
0.22 (LNCaP; Western)
0.39 (MDA-MB-468; Acumen)
pFOXO3a translocation0.69 (BT474c)

NOTE: In vitro kinase assays were conducted to determine the potency and selectivity of AZD5363 against Akt1, Akt2, Akt3, and other members of the AGC-kinase family. Cellular assays were used to show cellular potency against AKT substrates.