PQR530
| CAS No. | 1927857-61-1 | Cat. No. | BCP20879 |
| Name | PQR530 | ||
| Synonyms | PQR-0530; PQR 530; | ||
| Formula | C18H23F2N7O2 | M. Wt | 407.42 |
| Description | PQR530 is a highly potent dual pan-PI3K/mTORC1/2 inhibitor. PQR530 inhibited protein kinase B (PKB, pSer473) and ribosomal protein S6 (pS6, pSer235/236) phosphorylation with IC50 values of 0.07 µM. PQR530 showed excellent selectivity over a wide panel of kinases, as well as excellent selectivity versus unrelated receptor enzymes and ion channels. Moreover, PQR530 displayed potency in a panel of 44 cancer cell lines (NTRC OncolinesTM) to prevent cancer cell growth (mean value for GI50 of 426 nM). Oral application of PQR530 to mice resulted in a dose-proportional PK and demonstrated good oral bioavailability and excellent brain penetration. | ||
| Pathways | PI3K/Akt/mTOR | ||
| Targets | PI3K mTOR | ||
Structure
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