5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine Chemical Properties

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

5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine Usage And Synthesis

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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