PF-04802367 - 10mM in DMSO , CAS No.1962178-27-3

CAS: 1962178-27-3 Cat. No.: P654675 Formula: C₁₆H₁₆ClN₅O₃ Peso molecolare: 361.78 Numero EC: 110-369-0

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC 50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay. PF-04802367 shows desirable central nervous system (CNS) properties and potency. PF-04802367 is equally effective at inhibition of the two known GSK-3 isoforms ( GSK-3α and GSK-3β ) with IC 50 values of 10.0 and 9.0 nM in mobility shift assays, respectively

In Vitro

PF-04802367 (PF-367) is efficient at inhibiting GSK-3β enzymatic activity in vitro with ligand and lipophilic efficiency scores of 0.46 and 7.0, respectively. PF-367 has reasonable in vitro stability in human hepatic microsomes (t 1/2 =78.7 min), has excellent passive permeability. In a stable inducible CHO cell line over-expressing GSK-3β and its substrate tau, PF-367 inhibited phosphorylation of tau with an IC 50 of 466 nM. PF-367 has good cell viability (IC 50 of 117 μM in THLE cytotoxicity assays) and an IC 50 >100 μM in a hERG screening assay. PF-367 shows significant right shifts against β-catenin translocation in HeLa cells with EC 50 of 6.2 μM, gene transcription in U20S cells with EC 50 of 20.6 μM, and cell proliferation in HeLa cells as evaluated by Ki-67 incorporation with EC 50 of 9.0 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PF-04802367 (PF-367) a potent GSK-3 inhibitor with exceptional kinome selectivity that modulates phosphorylated tau levels in vivo. Inhibition of phosphorylation of tau in brain by PF-367 (A single subcutaneous of 1, 3.2, 10, 32 or 50 mg/kg) is dose-dependent . PF-04802367 (PF-367), a potent type-I dual GSK-3α/β inhibitor, showing promising absorption; distribution, metabolism and elimination (ADME) properties combined with robust CNS/peripheral p-Tau and muscle phosphorylated glycogen synthase (pGS) inhibition in vivo. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Sprague-Dawley rats Dosage: 1, 3.2, 10, 32 or 50 mg/kg Administration: A single subcutaneous Result: Inhibition of phosphorylation of tau in brain is dose-dependent.

IC50& Target:GSK-3α 10 nM (IC 50 ) GSK-3β 9 nM (IC 50 )

Specifications

Specifiche e purezza

10mM in DMSO

Meccanismi biochimici e fisiologici

PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC 50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay.xa0PF-04802367 shows desirable central nervous system (CNS)xa0properties and potency. PF-

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Tipo di azione

INHIBITOR

Nomi e identificatori

• Peso molecolare: 361.78

Domande frequenti

How should this product be stored?

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

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 are the CAS number, molecular formula and molecular weight?

The CAS Number is 1962178-27-3, the molecular formula is C16H16ClN5O3, and the molecular weight is 361.78 g/mol.

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.