PQR626 - 10mM in DMSO , CAS No.1927857-98-4

CAS: 1927857-98-4 Cat. No.: P656497 Summenformel: C₂₀H₂₇F₂N₇O₂ Molekulargewicht: 435.47 PubChem CID: 121334440

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

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 disorders

In Vitro

PQR626 (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 Vivo

PQR626 (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).

IC50& Target:IC50: 5 nM (mTOR)

Specifications

Spezifikationen & Reinheit

10mM in DMSO

Biochemische und physiologische Mechanismen

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 disorders.

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Aktionsart

INHIBITOR

Namen und Kennungen

• Isomere SMILES: C[C@@H]1COCCN1C2=NC(=NC(=N2)C3=CN=C(C=C3C(F)F)N)N4[C@@H](COC[C@@H]4C)C
• PubChem CID: 121334440
• Molekulargewicht: 435.47

Zugehörige Ziele (menschlich)

MTOR Tclin Serine/threonine-protein kinase mTOR (2 Activities)

Discover Target: MTOR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Häufig gestellte Fragen

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1927857-98-4, the molecular formula is C20H27F2N7O2, and the molecular weight is 435.47 g/mol.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.