Zabadinostat - 10mM in DMSO , CAS No.934828-12-3

CAS: 934828-12-3 Cat. No.: Z654839 Peso molecular: 403.5 PubChem CID: 16225380

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Zabadinostat (CXD101) is a potent, selective and orally active class I HDAC inhibitor with IC 50 s of 63 nM, 570 nM and 550 nM for HDAC1 , HDAC2 and HDAC3 , respectively. Zabadinostat has no activity against HDAC class II. Zabadinostat has antitumor activity

In Vitro

Zabadinostat has been tested in vitro in colon, lung, non-Hodgkin lymphoma, and myeloma cell lines with IC 50 s ranged from 0.2 to 15 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Zabadinostat substantially reduces tumor size in murine xenograft lung (A549a) and colon (HT29) models at a dose of 50 mg/kg. Tumor reductions are found to be associated with increased histone acetylation and decreased HDAC enzyme activity. For Zabadinostat, after oral dosing in murine and canine models, peak plasma concentrations (C max ) are reached 1 to 2 hours after the dose and terminal half‐lives are 6 hours and 8 hours, respectively. After murine oral [ 14 C]-Zabadinostat at a dose of 1.6 mg/kg (4 μmol/kg), tissue radioactivity peaked 3 to 6 hours after the dose and declined slowly thereafter with Zabadinostat‐related material still present in tissue 21 days after the dose. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:HDAC1 63 nM (IC 50 ) HDAC3 550 nM (IC 50 ) HDAC2 570 nM (IC 50 )

Specifications

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Zabadinostat (CXD101) is a potent, selective and orally active class I HDAC inhibitor with IC 50 s of 63 nM, 570 nM and 550 nM for HDAC1 , HDAC2 and HDAC3 , respectively. Zabadinostat has no activity against HDAC class II. Zabadinostat has antitumor activ

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Nombres e identificadores

• Isómeros SMILES: CC1=NN(C=C1CN2CCC(CC2)C3=CC=C(C=C3)C(=O)NC4=CC=CC=C4N)C
• CAS alternativo: 934828-12-3,1397710-94-9
• PubChem CID: 16225380
• Peso molecular: 403.5