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PQR530 Chemical Structure

PQR530

Data Sheet For research use only. Not for human use.
Cat. No. ：BCP20879CAS No. ：1927857-61-1Purity：98%
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  • Chemical Properties&Biological Activity
CAS No. 1927857-61-1 Cat. No. BCP20879
Name PQR530
Synonyms PQR-0530; PQR 530;
SMILES FC(C1=CC(N)=NC=C1C2=NC(N3CCOCC3)=NC(N4[C@](COCC4)C)=N2)F
Chemical Name
Formula C18H23F2N7O2 M. Wt 407.42
Purity 98% Storage Store at 4-8°C
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.
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