| Identification | Back Directory | [Name]
2-Pyridinamine, 4-(difluoromethyl)-5-[4-[(3R,5S)-3,5-dimethyl-4-morpholinyl]-6-[(3R)-3-methyl-4-morpholinyl]-1,3,5-triazin-2-yl]- | [CAS]
1927857-98-4 | [Synonyms]
PQR626
2-Pyridinamine, 4-(difluoromethyl)-5-[4-[(3R,5S)-3,5-dimethyl-4-morpholinyl]-6-[(3R)-3-methyl-4-morpholinyl]-1,3,5-triazin-2-yl]- | [Molecular Formula]
C20H27F2N7O2 | [MOL File]
1927857-98-4.mol | [Molecular Weight]
435.47 |
| Chemical Properties | Back Directory | [Boiling point ]
655.4±65.0 °C(Predicted) | [density ]
1.264±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
5.05±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Description]
PQR626 is a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Disorders. | [Uses]
PQR626, a rapamycin derivative, is a potent, selective, orally active, and brain-penetrant mTOR inhibitor, with an IC50 and Ki of 5 nM and 3.6 nM, respectively. PQR626 can be can be used for the research of neurological disorders[1][2]. | [in vivo]
PQR626 (10-50 mg/kg; twice a day; for 90 days) reduces the loss of Tsc1-induced mortality as compared to vehicle[2].
PQR626 exhibits terminal elimination half-life (mice 3.0 h) due to high plasma clearance (1096 ng/mL) following oral dosing (10 mg/kg; p.o.; daily; for 4 days)[2].
| Animal Model: | BALB/c nude female mice, Tsc1GFAP CKO mice model[2] | | Dosage: | 10 mg/kg, 25 mg/kg, 50 mg/kg | | Administration: | Oral administration, twice a day, for 90 days | | Result: | Significantly reduced the loss of Tsc1-induced mortality. |
| Animal Model: | Female C57BL/6J Mice[1] | | Dosage: | 10 mg/kg (Pharmacokinetic Analysis) | | Administration: | Oral administration, daily, for 4 days | | Result: | Cmax (1096 ng/mL), T1/2 (3.0 h). |
| [References]
[1] Denise RAGEOT, et al. Treatment of neurological disorders. WO2017198346A1.
[2] Chiara Borsari, et al. 4-(Difluoromethyl)-5-(4-((3 R,5 S)-3,5-dimethylmorpholino)-6-(( R)-3-methylmorpholino)-1,3,5-triazin-2-yl)pyridin-2-amine (PQR626), a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Disorders. J Med Chem. 2020 Nov 25;63(22):13595-13617. DOI:10.1021/acs.jmedchem.0c00620 |
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