HDAC-IN-4

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

组蛋白脱乙酰酶 (HDAC) 抑制剂。

A histone deacetylase (HDAC) inhibitor, extracted from patent WO/2007045844 A1.(In Vitro):Zabadinostat has been tested in vitro in colon, lung, non-Hodgkin lymphoma, and myeloma cell lines with IC50s ranged from 0.2 to 15 μM.(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 (Cmax) are reached 1 to 2 hours after the dose and terminal half‐lives are 6 hours and 8 hours, respectively. After murine oral [14C]-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.

Zabadinostat has been tested in vitro in colon, lung, non-Hodgkin lymphoma, and myeloma cell lines with IC50s ranged from 0.2 to 15 μM.

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 (Cmax) are reached 1 to 2 hours after the dose and terminal half‐lives are 6 hours and 8 hours, respectively. After murine oral [14C]-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.

AZD 9468

Cell Cycle/DNA Damage

HDAC

HDAC

Cancer

——

934828-12-3

403.52

C24H29N5O

>98% (HPLC)

DMSO: ≥ 31 mg/mL

O=C(NC1=CC=CC=C1N)C2=CC=C(C3CCN(CC4=CN(C)N=C4C)CC3)C=C2

Benzamide, N-(2-aminophenyl)-4-[1-[(1,3-dimethyl-1H-pyrazol-4-yl)methyl]-4-piperidinyl]-

(-20℃)

With Ice Pack

≥ 2 years