分子量

349.43

储存条件

3年-20°C 粉状
2年-80°C 溶于溶剂

化学式

C21H23N3O2

CAS号

404950-80-7

别名

NVP-LBH589

化学名

(E)-N-hydroxy-3-(4-((2-(2-methyl-1H-indol-3-yl)ethylamino)methyl)phenyl)acrylamide

Solubility (25°C) *

体外

DMSO

70 mg/mL (200.32 mM)

Water

Insoluble

Ethanol

Insoluble

体内（现配现用）

2% DMSO+48% PEG 300+2% Tween 80+ddH2O

5mg/mL

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

浓度 / 溶剂体积 / 质量

1 mg

5 mg

10 mg

1 mM

2.8618 mL

14.3090 mL

28.6180 mL

5 mM

0.5724 mL

2.8618 mL

5.7236 mL

10 mM

0.2862 mL

1.4309 mL

2.8618 mL

50 mM

0.0572 mL

0.2862 mL

0.5724 mL

产品描述

Panobinostat (LBH589, NVP-LBH589)是一种新型的，广谱HDAC抑制剂，无细胞试验中IC50为5 nM。Panobinostat (LBH589) 可诱导自噬和凋亡。Panobinostat 可以有效地破坏体内 HIV 的潜伏期。Phase 3。

靶点/IC50

HDAC, IC50: 5 nM~20 nM

体外研究

Panobinosta (LBH589) induces apoptosis of both MOLT-4 and Reh cells in a time- and dose-dependent manner. Panobinosta treatment results in histone (H3K9 and H4K8) hyperacetylation and regulation of cell-cycle control genes in Reh cells. Panobinostat exhibites potent antiproliferative activity in human NSCLC cell lines with the IC50 ranging from 5 to 100 nM.

体内研究

Panobinosta (10, 20 mg/kg, i.p.) significantly slows tumor growth derived from Meso and NSCLC cells in vivo models. Panobinosta markedly increases acetylation of histone H3 and H4 of H69 human SCLC cells harvest from SCID mice. Panobinostat (5, 10 and 20 mg/kg i.p.) demonstrates a clear benefit of decreased tumor burden, significantly improves TTE and reduces bone density loss in a disseminated multiple myeloma mouse model.

细胞系

MOLT-4细胞和Reh(前体B细胞)

浓度

50 nM

处理时间

48小时

方法

没有处理的细胞和LBH589处理的细胞[人类急性成淋巴细胞性白血病MOLT-4(T 细胞)和Reh(前体-B细胞)]用膜联蛋白V和碘化丙啶染色，然后加入膜联蛋白V-FITC细胞凋亡检测试剂盒I。通过流式细胞仪测定细胞凋亡和不能存活细胞的百分比。用CyAn ADP Violet细胞计数器收集至少5×104个细胞。根据所有的膜联蛋白V-阳性和膜联蛋白V/PI-阳性细胞细胞计算凋亡百分比，根据所有的膜联蛋白V-阳性和PI-阳性及膜联蛋白V/PI-阳性细胞计算细胞活力丢失百分比。