PQR626 (C007B-386422)

PQR626, a rapamycin derivative, is a potent, selective, orally active, and brain-penetrant mTOR inhibitor, with an IC 50 and K i of 5 nM and 3.6 nM, respectively. PQR626 can be can be used for the research of neurological disordersIn VitroPQR626 (0.04-5 μΜ; 1 hour) has IC 50 s 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: A2058 cells Concentration: 0.04 μΜ, 0.08 μΜ, 0.155 μΜ, 0.3125 μΜ, 0.625 μΜ, 1.25 μΜ, 5 μΜ Incubation Time: 1 hour Result: Inhibited mTOR in cell.In VivoPQR626 (10-50 mg/kg; twice a day; for 90 days) reduces the loss of Tsc1 -induced mortality as compared to vehicle. 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). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/c nude female mice, Tsc1 GFAP CKO mice modelDosage: 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 Dosage: 10 mg/kg (Pharmacokinetic Analysis) Administration: Oral administration, daily, for 4 days Result: C max (1096 ng/mL), T 1/2 (3.0 h).Form:SolidIC50& Target:IC50: 5 nM (mTOR). Specification: 0.98 Molecular Formula: C20H27F2N7O2 Molecular Weight: 435.47 PubChem CID: 121334440 Isomeric SMILES: C[C@@H]1COCCN1C2=NC(=NC(=N2)C3=CN=C(C=C3C(F)F)N)N4[C@@H](COC[C@@H]4C)C