For research use only. Not for therapeutic Use.
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].
PQR626 (0.04-5 μΜ; 1 hour) has IC50s of 197 nM and 87 nM for pPKB S473 and pS6 S235/S236, respectively, in-cell western blot. S6 kinase (S6K), S6 ribosomal protein (S6rP) and 4E-binding protein (4E-BP) are prominent downstream effectors of mTOR[1].
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].
| Catalog Number | I034981 |
| CAS Number | 1927857-98-4 |
| Synonyms | 4-(difluoromethyl)-5-[4-[(3S,5R)-3,5-dimethylmorpholin-4-yl]-6-[(3R)-3-methylmorpholin-4-yl]-1,3,5-triazin-2-yl]pyridin-2-amine |
| Molecular Formula | C20H27F2N7O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C20H27F2N7O2/c1-11-8-30-5-4-28(11)19-25-18(15-7-24-16(23)6-14(15)17(21)22)26-20(27-19)29-12(2)9-31-10-13(29)3/h6-7,11-13,17H,4-5,8-10H2,1-3H3,(H2,23,24)/t11-,12-,13+/m1/s1 |
| InChIKey | YXQKBQLVKBUCLZ-UPJWGTAASA-N |
| SMILES | CC1COCCN1C2=NC(=NC(=N2)C3=CN=C(C=C3C(F)F)N)N4C(COCC4C)C |
| Reference | [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 Dis |
