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

CAS NO.：1225037-39-7
Empirical Formula: C17H20F3N7O2
Molecular Weight: 411.38
MDL number: MFCD28902193
Update Date: 2024-07-02 08:55:16

What is 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine?

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.

The Uses of 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine

Bimiralisib is an orally bioavailable PI3K/mTOR inhibitor for cancer

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

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

Safety information for 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine

Computed Descriptors for 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine

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