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Quisinostat

JNJ-26481585,JNJ26481585,JNJ 26481585

Quisinostat (JNJ-26481585) is a novel second-generation HDACi inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7. , in NSCLC cells. In vitro, quisinostat has shown anti-proliferative activity against NSCLC cell lines. quisinostat extremely changed protein acetylation patterns of A549 cells and inhibited epithelial-mesenchymal transition (EMT) process.

目录号
EY2222
EY2222
EY2222
EY2222
纯度
99.21%
99.21%
99.21%
99.21%
规格
1 mg
5 mg
10 mg
50 mg
原价
445
1150
1750
4200
售价
445
1150
1750
4200
库存
现货
现货
现货
现货
订购
订购
订购
订购
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  • 生物活性

    Quisinostat (JNJ-26481585) is a novel second-generation HDACi inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7. , in NSCLC cells. In vitro, quisinostat has shown anti-proliferative activity against NSCLC cell lines. quisinostat extremely changed protein acetylation patterns of A549 cells and inhibited epithelial-mesenchymal transition (EMT) process. Exposure to quisinostat induced mitochondrial injury and increased p53 acetylation, resulting in cell apoptosis and G1 phase arrest. In conclusion, these findings provide the proof of concept for evaluation of quisinostat as a novel NSCLC chemotherapeutic agent. Phase 2.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Hernan Carol, et al. Initial Testing (Stage 1) of the histone deacetylase inhibitor, quisinostat (JNJ-26481585), by the Pediatric Preclinical Testing Program. Pediatr Blood Cancer. Author manuscript; available in PMC 2015 Feb 1. Published in final edited form as: Pediatr Blood Cancer. 2014 Feb; 61(2): 245–252. Published online 2013 Sep 4. doi: 10.1002/pbc.24724.

    分子式
    C21H28Cl2N6O2    		 分子量
    394.48    		 CAS号
    875320-31-3    		 储存方式
    -20 ℃长期冷藏储存。冰袋运输
    溶剂（常温）
    		 DMSO
    76 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度
    15% Captisol 30 mg/mL

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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