Identification | Back Directory | [Name]
5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine | [CAS]
1225037-39-7 | [Synonyms]
PQR309 CS-2024 PI3K-IN-2 Bimiralisib PQR-309, >98% PQR309 Bimiralisib Bimiralisib (PQR309) PQR309;PQR 309;PQR-309 Bimiralisib (PQR309)(free base) BIMIRALISIB;PQR309;PQR 309;PQR-309 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine 2-Pyridinamine,5-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)-4-(trifluoromethyl)- | [Molecular Formula]
C17H20F3N7O2 | [MDL Number]
MFCD28902193 | [MOL File]
1225037-39-7.mol | [Molecular Weight]
411.38 |
Chemical Properties | Back Directory | [Boiling point ]
643.7±65.0 °C(Predicted) | [density ]
1.418±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:22.0(Max Conc. mg/mL);53.48(Max Conc. mM) DMF:10.0(Max Conc. mg/mL);24.31(Max Conc. mM) Ethanol:2.0(Max Conc. mg/mL);4.86(Max Conc. mM) | [form ]
A crystalline solid | [pka]
4.92±0.10(Predicted) | [color ]
White to gray |
Hazard Information | Back Directory | [Description]
Bimiralisib is a potent and orally bioavailable inhibitor of phosphatidylinositol 3-kinases (PI3Ks; IC50s = 33, 661, 708, and 451 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively) and the mammalian target of rapamycin (mTOR; IC50 = 89 nM). It is selective for these kinases over a panel of cell surface and nuclear receptors, membrane channels, transporters, kinases, proteases, and phosphodiesterases at a concentration of 10 μM. Bimiralisib has anticancer activity with an average GI50 value of 0.7 μM across the National Cancer Institute (NCI) 60 human cancer cell line panel. In vivo, bimiralisib (5-15 mg/kg) reduces tumor growth in a dose-dependent manner in a PC3 prostate cancer mouse xenograft model. Formulations containing bimiralisib are under clinical investigation for the treatment of relapsed and refractory lymphoma and advanced solid tumors. | [Uses]
Bimiralisib is an orally bioavailable PI3K/mTOR inhibitor for cancer |
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