Inhibitors of PI3K/PKB signaling pathway
| Target . | Compound . | Effect . | Clinical trials (phase) . | Leukemia . | Reference(s) . | |
|---|---|---|---|---|---|---|
| In vitro . | In vivo . | |||||
| PI3K | Wortmannin | + | − | 147,148 | ||
| LY294002 | + | − | 37,148,–150 | |||
| AS702630 | + | − | 105 | |||
| S14161 | + | + | 96 | |||
| p110β | TGX-115 | + | − | 36,105 | ||
| p110δ | IC87114 | + | − | 36,38,105,145 | ||
| AMG 319 | − | − | NCT01300026 (1) | CLL and ALL | ||
| CAL-101 | + | + | NCT01090414 (1) | CLL and AML | 80,98,99 | |
| + | + | NCT00710528 (1) | CLL and AML | 80,98,99 | ||
| PDK1 | UCN-01 | + | − | 122 | ||
| PKB | Perifosine | + | − | NCT00391560 (2) | RRL | 101,–103 |
| − | − | NCT00873457 (2) | CLL | |||
| PIA | + | − | 104 | |||
| A-443654 | + | − | 53 | |||
| AiX | + | − | 107 | |||
| Triciribine (API-2) | + | − | NCT00363454 (1) | 106 | ||
| AKT-I-1/2 | + | − | 52,53 | |||
| GSK690693 | + | − | NCT00493818 (1) | 151 | ||
| MK2206 | − | − | NCT01231919 (1) | RRL | ||
| − | − | NCT01253447 (2) | AML | |||
| SR13668 | − | − | NCT00896207 (1) | |||
| GSK2141795 | − | − | NCT00920257 (1) | |||
| GSK21110183 | − | − | NCT00881946 (1/2) | RRL | ||
| mTOR | Rapamycin | + | + | NCT00795886 (2) | ALL | 112,152,153 |
| + | + | NCT00068302 (1) | ALL and AML | 112,152,153 | ||
| + | + | (2) | CML | 154,155 | ||
| RAD001 | + | + | NCT00636922 (1) (1/2) | AML AML and MDS | 138 | |
| + | + | (2) | B-CLL | 109 | ||
| + | + | (2) | CLL | 116 | ||
| CCI-779 | + | + | NCT00290472 (2) | CLL | ||
| + | + | NCT00084916 (2) | RRL | |||
| + | + | NCT00084474 (2) | CLL | |||
| + | + | (2) | ALL | 156 | ||
| AP23573 | − | − | (2) | AML | 113 | |
| NCT00086125 (2) | RRL | |||||
| PP242 | + | + | 117,118,157 | |||
| OSI-027 | + | − | 118,–120 | |||
| AZD-8050 | + | − | 118 | |||
| PI3K/mTOR | PI-103 | + | + | 76,126,127,158 | ||
| NVP-BEZ235 | + | + | 123,–125 | |||
| PI3K/PDK1 | BAG956 | + | + | 121 | ||
| PKB/PDK1/Flt3 | KP372-1 | + | − | 128 | ||
| Target . | Compound . | Effect . | Clinical trials (phase) . | Leukemia . | Reference(s) . | |
|---|---|---|---|---|---|---|
| In vitro . | In vivo . | |||||
| PI3K | Wortmannin | + | − | 147,148 | ||
| LY294002 | + | − | 37,148,–150 | |||
| AS702630 | + | − | 105 | |||
| S14161 | + | + | 96 | |||
| p110β | TGX-115 | + | − | 36,105 | ||
| p110δ | IC87114 | + | − | 36,38,105,145 | ||
| AMG 319 | − | − | NCT01300026 (1) | CLL and ALL | ||
| CAL-101 | + | + | NCT01090414 (1) | CLL and AML | 80,98,99 | |
| + | + | NCT00710528 (1) | CLL and AML | 80,98,99 | ||
| PDK1 | UCN-01 | + | − | 122 | ||
| PKB | Perifosine | + | − | NCT00391560 (2) | RRL | 101,–103 |
| − | − | NCT00873457 (2) | CLL | |||
| PIA | + | − | 104 | |||
| A-443654 | + | − | 53 | |||
| AiX | + | − | 107 | |||
| Triciribine (API-2) | + | − | NCT00363454 (1) | 106 | ||
| AKT-I-1/2 | + | − | 52,53 | |||
| GSK690693 | + | − | NCT00493818 (1) | 151 | ||
| MK2206 | − | − | NCT01231919 (1) | RRL | ||
| − | − | NCT01253447 (2) | AML | |||
| SR13668 | − | − | NCT00896207 (1) | |||
| GSK2141795 | − | − | NCT00920257 (1) | |||
| GSK21110183 | − | − | NCT00881946 (1/2) | RRL | ||
| mTOR | Rapamycin | + | + | NCT00795886 (2) | ALL | 112,152,153 |
| + | + | NCT00068302 (1) | ALL and AML | 112,152,153 | ||
| + | + | (2) | CML | 154,155 | ||
| RAD001 | + | + | NCT00636922 (1) (1/2) | AML AML and MDS | 138 | |
| + | + | (2) | B-CLL | 109 | ||
| + | + | (2) | CLL | 116 | ||
| CCI-779 | + | + | NCT00290472 (2) | CLL | ||
| + | + | NCT00084916 (2) | RRL | |||
| + | + | NCT00084474 (2) | CLL | |||
| + | + | (2) | ALL | 156 | ||
| AP23573 | − | − | (2) | AML | 113 | |
| NCT00086125 (2) | RRL | |||||
| PP242 | + | + | 117,118,157 | |||
| OSI-027 | + | − | 118,–120 | |||
| AZD-8050 | + | − | 118 | |||
| PI3K/mTOR | PI-103 | + | + | 76,126,127,158 | ||
| NVP-BEZ235 | + | + | 123,–125 | |||
| PI3K/PDK1 | BAG956 | + | + | 121 | ||
| PKB/PDK1/Flt3 | KP372-1 | + | − | 128 | ||
RRL indicates relapsed and refractory leukemia.