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CAS No.: 875320-31-3

Quisinostat 2HCl Catalog No. CSN18839

Synonyms: JNJ-26481585 dihydrochloride;JNJ-26481585 2HCl;JNJ-26481585

Quisinostat 2HCl is a 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.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 HDAC1

IC50:0.11nM HDAC10

IC50:0.46nM HDAC11

IC50:0.37nM HDAC2

IC50:0.33nM HDAC3

IC50:4.86nM 更多
描述The inhibition of HDACs increases the acetylation of histone proteins, which affects the tertiary chromatin structure and leads to altered expression of genes involved in cell proliferation, apoptosis and differentiation. Thus, it makes a key role for inhibition of HDACs in anti-proliferation of tumor cells. Quisinostat is an oral pan-HDAC inhibitor with highest potency for HDAC1 (IC50=0.11±0.03nM, measured by recombinant HDAC enzyme activity), modest potent to HDAC 2, 4, 10 and 11nM and a lower potency on the rest HDACs. Increased level of acetylated histone H3 (H3 Ac), H4 (H4 Ac), histone H4-acetyl K16 (H4-K16 Ac) and histone H4-trimethyl K20 (H4-K20Me3) (acetylation regulated by HDAC1-3), p21 and E-cadherin (expression regulated by HDAC1), as well as increased tubulin acetylation, induction of Hsp70, and loss of Hsp90 client c-Raf can be observed in a dose-dependent manner (30-1000nM) after 24-hour treatment with Quisinostat in human A2780 ovarian carcinoma cells, which shows activity against pan-HDAC inhibition. Also, Quisinostat can inhibit cell growth in all lung, breast, colon, prostate, brain, and ovarian tumor cell lines tested with IC50 values ranging from 3.1 to 246nM, which shows its antiproliferative effect in a broad panel of human tumor cell lines from both solid and hematologic origin. Compared with the first generation of HDAC inhibitors (SAHA or TSA), Quisinostat shows prolonged pharmacodynamic response in vivo. Quisinostat can induce continuous H3 acetylation in tumor tissue from A2780 ovarian tumor-bearing nude mice when treated with Quisinostat at 10mg/kg as well as increased level of HDAC1-regulated p21^[1]. Up to now, a phase I study of Quisinostat in patients with advanced solid tumors has been done^[2].
作用机制Quisinostat is a pyrimidyl-hydroxamic acid analogue, which can chelate the Zn²⁺ ion of HDAC. ^[1]

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1395 mL
- 10.6977 mL
- 21.3953 mL
- 5 mM
- 0.4279 mL
- 2.1395 mL
- 4.2791 mL
- 10 mM
- 0.2140 mL
- 1.0698 mL
- 2.1395 mL

技术信息

CAS号

875320-31-3

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H28Cl2N6O2

运输

蓝冰

分子量

467.39

别名

JNJ-26481585 dihydrochloride;JNJ-26481585 2HCl;JNJ-26481585;JNJ-26481585-AAC;Quisinostat HCl;Quisinostat hydrochloride;quisinostat dihydrochloride

溶解度

DMSO	375.0 mg/mL (802.3 mM) warming
Water	3.0 mg/mL (6.4 mM) warming

动物实验配方

IP	2% DMSO+water	7 mg/mL	clear
PO	0.5% CMC-Na	40 mg/mL	suspension

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靶点	Description	IC50
HDAC1		IC50:0.11nM
HDAC10		IC50:0.46nM
HDAC11		IC50:0.37nM
HDAC2		IC50:0.33nM
HDAC3		IC50:4.86nM
HDAC4		IC50:0.64nM
HDAC5		IC50:3.69nM
HDAC8		IC50:4.26nM

Quisinostat 2HCl Catalog No. CSN18839

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