Table 1. A674563 anti-proliferative efficacy against FLT3-ITD positive/wt intact cancer cell lines A.
Drug/Cell line GI50(μM) | A674563 | AZD5363 | CCT128930 | GDC0068 | GSK690693 | MK2206 | TCS359 | AC220 |
---|---|---|---|---|---|---|---|---|
(Primary target) | (AKT) | (AKT) | (AKT) | (AKT) | (AKT) | (AKT) | (FLT3) | (FLT3) |
MOLM-13 (FLT3-ITD/wt) |
0.06 | 0.16 | 0.65 | 0.29 | 0.28 | 0.1 | 0.56 | < 0.0003 |
MV4-11 (FLT3-ITD) |
0.075 | 0.67 | 1 | 2.1 | 5.2 | 5.2 | 0.68 | < 0.0003 |
MOLM-14 (FLT3-ITD/wt) |
0.18 | 0.5 | 1.1 | 0.85 | 0.54 | 0.32 | 10-3 | < 0.0003 |
OCI-AML-3 (FLT3-wt) |
0.67 | 1.2 | 2.2 | 1.1 | > 10 | 1.4 | > 10 | 3–1 |
U937 (FLT3-wt) |
0.52 | 0.61 | 4.1 | 0.59 | 5.1 | 7.2 | > 10 | 0.94 |
NB4 (FLT3-wt) |
0.48 | 0.93 | 2.5 | 5.9 | 0.22 | 0.21 | > 10 | > 10 |
HL-60 (FLT3-wt) |
2.6 | 0.37 | 1.5 | 0.31 | 0.16 | 0.16 | 0.54 | 0.55 |
PF-382 (FLT3-wt) |
2.7 | 0.48 | 1.3 | 0.44 | 0.24 | 0.61 | > 10 | 0.49 |
SKM-1 (FLT3-wt) |
2 | > 10 | 4.3 | > 10 | > 10 | 4.6 | > 10 | 1.3 |