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Quisinostat dihydrochloride

产品编号 T6865 CAS 875320-31-3

别名: Quisinostat 2HCl, Quisinostat (JNJ-26481585) 2HCl, JNJ26854165(Quisinostat) 2HCl, JNJ-26481585 2HCl

Quisinostat dihydrochloride (JNJ26854165(Quisinostat) 2HCl) 是一种有口服活性，高效的 pan-HDAC 抑制剂，具有广泛的抗肿瘤活性。它对 HDAC1、HDAC2、HDAC4、HDAC10和HDAC11 的IC50值分别为 0.11 nM、0.33 nM、0.64 nM、0.46 nM 和 0.37 nM。

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Quisinostat dihydrochloride Chemical Structure

Quisinostat dihydrochloride, CAS 875320-31-3

规格	价格/CNY	货期
1 mg	￥ 372	现货
5 mg	￥ 997	现货
10 mg	￥ 1,490	现货
25 mg	￥ 2,480	现货
50 mg	￥ 3,570	现货
100 mg	￥ 4,970	现货
1 mL * 10 mM (in DMSO)	￥ 987	现货

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其他形式的 Quisinostat dihydrochloride:

Quisinostat
现货

选择批次

纯度: 98.5%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Quisinostat dihydrochloride (JNJ26854165(Quisinostat) 2HCl) is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM in a cell-free assay, 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. Phase 2.
靶点活性	HDAC1:0.11 nM
体外活性	JNJ-26481585 exhibits broad spectrum antiproliferative activity in solid and hematologic cancer cell lines, such as all lung, breast, colon, prostate, brain, and ovarian tumor cell lines, with IC50 ranging from 3.1-246 nM, which is more potent than vorinostat, R306465, panobinostat, CRA-24781, or mocetinostat in various human cancer cell lines tested. [1] A recent study shows that JNJ-26481585 promotes myeloma cell death at low nanomolar concentrations by resulting in Mcl-1 depletion and Hsp72 induction. [2]
体内活性	In an HDAC1-responsive A2780 ovarian tumor screening model, JNJ-26481585 dosing at its maximal tolerated dose (10 mg/kg i.p. and 40 mg/kg p.o.) for 3 days leads to an HDAC1-regulated fluorescence , which predicts tumor growth inhibition. Furthermore, JNJ-26481585 also shows more potent inhibitory effects on the growth of C170HM2 colorectal liver metastases than 5-fluorouracil/Leucovorin. [1]
激酶实验	HDAC activity assays : In all cases, full-length HDAC proteins are expressed using baculovirus-infected Sf9 cells. In addition, HDAC3 is coexpressed as a complex with human NCOR2. For assessing activity of HDAC1-containing cellular complexes, immunoprecipitated HDAC1 complexes are incubated with an [3H]acetyl- labeled fragment of histone H4 peptide [biotin-(6-aminohexanoic)Gly-Ala-(acetyl[3H])Lys-Arg-His-Arg-Lys-Val-NH2] in a total volume of 50μL enzyme assay buffer (25 mM HEPES (pH 7.4), 1 M sucrose, 0.1 mg/mL BSA and 0.01% (v/v) Triton X-100). Incubation is performed for 45 minutes at 37 °C (immunoprecipitates) or 30 min at room temperature. Before addition of substrate, HDAC inhibitors are added at increasing concentrations and preincubated for 10 minutes at room temperature. After incubation, the reaction is quenched with 35μL stop buffer (1 M HCl and 0.4 M acetic acid). Released [3H]acetic acid is extracted with 800μL ethyl acetate and quantified by scintillation counting. Equal amounts of HDAC1 are immunoprecipitated as indicated by Western blot analysis. HDAC1 activity results are presented as mean ± SD of three independent experiments on a single lysate.
细胞实验	All cell lines are obtained from American Type Culture Collection and cultured according to instructions. The effect of HDAC inhibitors on cell proliferation is measured using an MTT. Proliferation of non–small cell lung carcinoma (NSCLC) cell lines is assessed using an Alamar Blue–based assay. For proliferation of hematologic cell lines, cells are incubated for 72 hours and the cytotoxic activity is evaluated by MTS assay. Data are presented as mean IC50 or IC40 ± SD of at least three independent experiments.(Only for Reference)

别名	Quisinostat 2HCl, Quisinostat (JNJ-26481585) 2HCl, JNJ26854165(Quisinostat) 2HCl, JNJ-26481585 2HCl
分子量	467.39
分子式	C21H28Cl2N6O2
CAS No.	875320-31-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 73 mg/mL (156.2 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1395 mL	10.6977 mL	21.3954 mL	53.4885 mL
	5 mM	0.4279 mL	2.1395 mL	4.2791 mL	10.6977 mL
	10 mM	0.214 mL	1.0698 mL	2.1395 mL	5.3489 mL
	20 mM	0.107 mL	0.5349 mL	1.0698 mL	2.6744 mL
	50 mM	0.0428 mL	0.214 mL	0.4279 mL	1.0698 mL
	100 mM	0.0214 mL	0.107 mL	0.214 mL	0.5349 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Arts J, et al. Clin Cancer Res, 2009, 15(22), 6841-6851. 2. Stühmer T, et al. Br J Haematol 2010, 149(4), 529-536

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Quisinostat dihydrochloride 875320-31-3 Apoptosis Autophagy Chromatin/Epigenetic DNA Damage/DNA Repair HDAC Histone deacetylases deacetylase Quisinostat JNJ26481585 Quisinostat 2HCl JNJ26854165(Quisinostat) histone Quisinostat (JNJ-26481585) 2HCl inhibit JNJ26854165(Quisinostat) 2HCl Inhibitor Quisinostat Dihydrochloride malignancies JNJ-26481585 2HCl hematologic JNJ-26481585 Quisinostat (JNJ-26481585) JNJ 26481585 inhibitor

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Quisinostat dihydrochloride

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords