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Belinostat

(Synonyms: 贝利司他; PXD101; PX105684)

目录号: PL14922 纯度: ≥99%

Belinostat (PXD101; PX105684) 是一种有效的 HDAC 抑制剂，在 HeLa 细胞提取物中的 IC50 为 27 nM。

CAS No. :866323-14-0

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中文名称	Belinostat
中文别名	贝利司他;(E)-N-羟基-3-[3-(N-苯基氨磺酰基)苯基]丙烯酰胺;(E)-N-羟基-3-(3-(N-苯基磺胺基)苯基)丙烯酰胺
英文名称	Belinostat
英文别名	2-Propenamide, N-hydroxy-3-[3-[(phenylamino)sulfonyl]phenyl]-, (2E)-;Belinostat;N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide;PX105684;PX-105684;PXD101;PXD-101;(E)-N-Hydroxy-3-[3-(N-phenylsulfamoyl)phenyl]acrylamide;Belinostat (PXD101);Beleodaq;NSC726630;(E)-N-hydroxy-3-(3-(N-phenylsulfamoyl)phenyl)acrylamide;PXD 101;N-HYDROXY-3-(3-PHENYLSULFAMOYLPHENYL)ACRYLAMIDE;PX 105684;F4H96P17NZ;(2E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide;(E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide;Belinostat(Random Configuration);(2E)-N-hydro
Cas No.	866323-14-0
分子式	C₁₅H₁₄N₂O₄S
分子量	318.35
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Belinostat (PXD101; PX105684) 是一种有效的 HDAC 抑制剂，在 HeLa 细胞提取物中的 IC₅₀ 为 27 nM。

生物活性

Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC 50 of 27 nM in HeLa cell extracts.

性状

Solid

IC50 & Target[1][2]

HDAC6 82 nM (IC50) HDAC 27 nM (IC50

体外研究(In Vitro)

Belinostat (PXD101) induces a concentration-dependent (0.2-5 μM) increase in acetylation of histone H4 in tumor cell lines. Belinostat is cytotoxic in vitro in a number of tumor cell lines with IC50s in the range 0.2-3.4 μM as determined by a clonogenic assay and induces apoptosis. Belinostat inhibits the growth of a number of human tumor cell lines in vitro with IC50s determined by a clonogenic assay in the range 0.2-3.4 μM. Belinostat (PXD101) is a potent histone deacetylase (HDAC) inhibitor, potently inhibits the enzymatic activity of purified recombinant HDAC6 (IC50 of 82 nM). has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Treatment of nude mice bearing human ovarian and colon tumor xenografts with Belinostat (10-40 mg/kg/day i.p.) daily for 7 days causes a significant dose-dependent growth delay with no obvious signs of toxicity to the mice. Growth delay is also observed for xenografts of cisplatin-resistant ovarian tumor cells. A marked increase in acetylation of H4 is detected in blood and tumor of mice 3 h after treatment with Belinostat (PXD101). The inhibition of growth of human tumor xenografts in mice, with no apparent toxicity. Belinostat (PXD101) displays single-agent antitumor activity on human A2780 ovarian cancer s.c. xenografts which is enhanced via combination therapy with Carboplatin. 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

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Plumb JA, et al. Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histonedeacetylase inhibitor PXD101. Mol Cancer Ther. 2003 Aug;2(8):721-8.
[2]. Qian X, et al. Activity of PXD101, a histone deacetylase inhibitor, in preclinical ovarian cancer studies. Mol Cancer Ther. 2006 Aug;5(8):2086-95.

溶解度数据	In Vitro: DMSO : 100 mg/mL (314.12 mM; Need ultrasonic)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。

Belinostat

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