| Identification | Back Directory | [Name]
2-Pyrimidinamine, 4-(difluoromethyl)-5-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)- | [CAS]
1927857-55-3 | [Synonyms]
2-Pyrimidinamine, 4-(difluoromethyl)-5-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)- | [Molecular Formula]
C16H20F2N8O2 | [MOL File]
1927857-55-3.mol | [Molecular Weight]
394.38 |
| Hazard Information | Back Directory | [Description]
PQR514 is a potent pan-PI3K inhibitor (Ki 110alpha =2.2 nM). PQR514 is a follow-up compound for the phase-II clinical compound PQR309. PQR514 has an improved potency both in vitro and in cellular assays with respect to its predecessor compounds. It shows superiority in the suppression of cancer cell_x000D_
proliferation and demonstrates significant antitumor activity in an OVCAR-3 xenograft model at concentrations approximately eight times lower than PQR309 | [Uses]
PQR514 is a potent PI3K inhibitor with anticancer activity. PQR514 is able to inhibit cancer cell proliferation. PQR514 showed significant antitumor activity in the OVCAR-3 xenograft model, with the required concentration being approximately one-eighth that of PQR309. PQR514 has good pharmacokinetic properties and minimal brain penetration, making it an optimized candidate compound for inhibiting systemic tumors[1]. | [References]
[1] Preclinical Development of PQR514, a Highly Potent PI3K Inhibitor Bearing a Difluoromethyl-Pyrimidine Moiety DOI:10.1021/acsmedchemlett.9b00333 |
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