Quisinostat dihydrochloride|875320-31-3|(JNJ-26481585 dihydrochloride)-陌孚医药/Medlife

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Quisinostat dihydrochloride (Synonyms: JNJ-26481585 dihydrochloride)

目录号: PL04429 纯度: ≥98%

CAS No. :875320-31-3

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中文名称	Quisinostat dihydrochloride
英文名称	Quisinostat dihydrochloride
英文别名	Quisinostat 2HCl;Quisinostat dihydrochloride;Quisinostat diHCl;BCP20792;SB16529;S1096;N-hydroxy-2-(4-((((1-methyl-1H-indol-3-yl)methyl)amino)methyl)piperidin-1-yl)pyrimidine-5-carboxamide dihydrochloride
Cas No.	875320-31-3
分子式	C₂₁H₂₈Cl₂N₆O₂
分子量	467.39
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Quisinostat dihydrochloride (JNJ-26481585 dihydrochloride) 是一种有口服活性，高效的 pan-HDAC 抑制剂，对 HDAC1，HDAC2，HDAC4，HDAC10，HDAC11 的 IC₅₀ 值分别为 0.11 nM，0.33 nM，0.64 nM，0.46 nM 和 0.37 nM。Quisinostat dihydrochloride 具有广泛的抗肿瘤活性。

生物活性

Quisinostat dihydrochloride (JNJ-26481585 dihydrochloride) is an orally available, potent pan-HDAC inhibitor with IC 50 s of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM, and 0.37 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11, respectively. Quisinostat dihydrochloride has a broad spectrum antitumoral activity.

性状

Solid

IC50 & Target[1][2]

HDAC1 0.11 nM (IC50) HDAC2 0.33 nM (IC

体外研究(In Vitro)

JNJ-26481585 inhibits HDAC isozymes in vitro.
JNJ-26481585 (30-1000 nM; 24 hours) is a potent pan-HDAC inhibitor in tumor cells.
JNJ-26481585 has broad spectrum antiproliferative activity against solid and hematologic cancer cell lines and induces apoptosis.
has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis

体内研究(In Vivo)

JNJ-26481585 (40 mg/kg; p.o.; once daily, for 3 days) as a potent HDAC1 inhibitor p21waf1,cip1 ZsGreen tumors in vivo.
JNJ-26481585 induces continuous H3 acetylation in tumor tissue in vivo.
JNJ-26481585 (10 mg/kg; once daily; i.p.; for 14 days) strongly inhibits the growth of large pre-established HCT116 colon xenografts.
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Arts J, et al. JNJ-26481585, a novel "second-generation" oral histone deacetylase inhibitor, shows broad-spectrum preclinical antitumoral activity. Clin Cancer Res. 2009 Nov 15;15(22):6841-51.

溶解度数据	In Vitro: DMSO : 31.25 mg/mL (66.86 mM; ultrasonic and warming and heat to 70°C)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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