Quisinostat dihydrochloride(Synonyms: JNJ-26481585 dihydrochloride)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Quisinostat dihydrochloride (Synonyms: JNJ-26481585 dihydrochloride)

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。

Quisinostat dihydrochloride(Synonyms: JNJ-26481585 dihydrochloride)

Quisinostat dihydrochloride Chemical Structure

CAS No. : 875320-31-3

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Quisinostat dihydrochloride 的其他形式现货产品:

Quisinostat

生物活性

Quisinostat dihydrochloride (JNJ-26481585 dihydrochloride) is an orally available, potent pan-HDAC inhibitor with IC50s 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[1].

IC50 & Target[1]

HDAC1

0.11 nM (IC50)

HDAC2

0.33 nM (IC50)

HDAC11

0.37 nM (IC50)

HDAC10

0.46 nM (IC50)

HDAC5

3.69 nM (IC50)

HDAC8

4.26 nM (IC50)

HDAC3

4.86 nM (IC50)

HDAC9

32.1 nM (IC50)

HDAC6

76.8 nM (IC50)

HDAC7

119 nM (IC50)

体外研究
(In Vitro)

JNJ-26481585 inhibits HDAC isozymes in vitro[1].
JNJ-26481585 (30-1000 nM; 24 hours) is a potent pan-HDAC inhibitor in tumor cells[1].
JNJ-26481585 has broad spectrum antiproliferative activity against solid and hematologic cancer cell lines and induces apoptosis[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Human A2780 ovarian carcinoma cells
Concentration: 30 nM, 100 nM, 300 nM, 1000 nM
Incubation Time: 24 hours
Result: Induced H3 and H4 acetylation at concentrations as low as 30 to 100 nM.

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[1].
JNJ-26481585 induces continuous H3 acetylation in tumor tissue in vivo[1].
JNJ-26481585 (10 mg/kg; once daily; i.p.; for 14 days) strongly inhibits the growth of large pre-established HCT116 colon xenografts[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NMRI nude mice, with HCT116 colon carcinoma cells xenografts[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection, once daily, for 14 days
Result: Strongly inhibited the growth of large pre-established HCT116 colon xenografts.

Clinical Trial

分子量

467.39

Formula

C21H28Cl2N6O2
CAS 号

875320-31-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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.

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