PQR530
- Catalog NO.:A903446
- CAS No. : 1927857-61-1
- Molecular Formula:C18H23F2N7O2
- Molecular Weight: 407.43
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Product Details
CAS Number | 1927857-61-1 | Appearance | |
Catalog Number | A903446 | MDL Number | |
Molecular Formula | C18H23F2N7O2 | Molecular Weight | 407.43 |
Boiling Point | Melting Point | ||
Flash Point | Density | ||
Synonyms | (S)-4-(difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine | ||
Storage Condition | Store in a tightly closed container,in a cool and dry place |
Safety
GHS Pictogram | |||
Signal Word | Warning | UN Number | |
Hazard Statements | Class | ||
Precautionary Statements | Packing Group |
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. |