Zabadinostat (C007B-433658)

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 activityIn VitroZabadinostat 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 VivoZabadinostat 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.Form:SolidIC50& Target:HDAC1 63 nM (IC 50 ) HDAC3 550 nM (IC 50 ) HDAC2 570 nM (IC 50 ). Specification: 0.99 Molecular Formula: C24H29N5O Molecular Weight: 403.5 PubChem CID: 16225380 Isomeric SMILES: CC1=NN(C=C1CN2CCC(CC2)C3=CC=C(C=C3)C(=O)NC4=CC=CC=C4N)C