AR-42

更新时间：2024-01-19 10:27:24

AR-42结构式	常用名	AR-42	英文名	AR-42
	CAS号	935881-37-1	分子量	312.36300
	密度	1.223	沸点	N/A
	分子式	C₁₈H₂₀N₂O₃	熔点	N/A
	MSDS	N/A	闪点	N/A

AR-42作用

体内：HDAC42有效抑制U87MG和PC-3细胞的增殖，部分原因在于其下调Akt信号传导的能力。 AR-42抑制PC-3和LNCaP细胞的生长，IC50分别为0.48μM和0.3μM。与SAHA相比，AR-42表现出明显优越的凋亡效力，并且导致PC-3细胞中磷酸-Akt，Bcl-xL和存活蛋白的显着降低。 AR-42处理诱导恶性肥大细胞系中的生长抑制，细胞周期停滞，细胞凋亡和胱天蛋白酶-3/7的活化。 AR-42处理通过抑制Kit转录，Kit和热休克蛋白90（HSP90）之间的解离以及HSP70的上调来诱导Kit的下调。 AR-42处理下调p-Akt，总Akt，磷酸化STAT3 / 5（pSTAT3 / 5）和总STAT3 / 5的表达。体外：在小鼠前列腺（TRAMP）模型的转基因腺癌中，给予AR-42不仅可以降低前列腺上皮内瘤变（PIN）的严重程度，并且可以完全阻止其进展为低分化癌，还可以将肿瘤发生转变为更多分化表型，分别抑制绝对和相对泌尿生殖道重量86％和85％。 AR-42显着降低了白细胞计数，并延长了B细胞恶性肿瘤的三个独立小鼠模型的存活率，没有毒性证据。

中文名	(S)-(+)-N-羟基-4-(3-甲基-2-苯基丁酰氨基)苯甲酰胺
英文名	N-hydroxy-4-[[(2S)-3-methyl-2-phenylbutanoyl]amino]benzamide
英文别名	更多

描述
相关类别	研究领域 >> 癌症
参考文献	[1]. Lu YS, Chou CH, Tzen KY, Gao M, Cheng AL, Kulp SK, Cheng JC.Radiosensitizing effect of a phenylbutyrate-derived histone deacetylase inhibitor in hepatocellular carcinoma.Int J Radiat Oncol Biol Phys. 2012 Jun 1;83(2):e181-9. Epub 2012 Feb 28. [2]. Zimmerman B, Sargeant A, Landes K, Fernandez SA, Chen CS, Lairmore MD.Efficacy of novel histone deacetylase inhibitor, AR42, in a mouse model of, human T-lymphotropic virus type 1 adult T cell lymphoma.Leuk Res. 2011 Nov;35(11):1491-7. Epub 2011 Jul 29. [3]. Zhang S, Suvannasankha A, Crean CD, White VL, Chen CS, Farag SS.The novel histone deacetylase inhibitor, AR-42, inhibits gp130/Stat3 pathway and induces apoptosis and cell cycle arrest in multiple myeloma cells.Int J Cancer. 2011 Jul 1;129(1):204-13. [4]. Lin TY et al. AR-42, a novel HDAC inhibitor, exhibits biologic activity against malignant mast cell lines via down-regulation of constitutively activated Kit. Blood. 2010 May 27;115(21):4217-25. [5]. Shuhong Zhang et al. The novel histone deacetylase inhibitor, AR-42, inhibits gp130/Stat3 pathway and induces apoptosis and cell cycle arrest in multiple myeloma cells International Journal of Cancer Volume 129, Issue 1, pages 204-213, 1 July 2011

描述

相关类别

研究领域 >> 癌症

参考文献

[1]. Lu YS, Chou CH, Tzen KY, Gao M, Cheng AL, Kulp SK, Cheng JC.Radiosensitizing effect of a phenylbutyrate-derived histone deacetylase inhibitor in hepatocellular carcinoma.Int J Radiat Oncol Biol Phys. 2012 Jun 1;83(2):e181-9. Epub 2012 Feb 28.

[2]. Zimmerman B, Sargeant A, Landes K, Fernandez SA, Chen CS, Lairmore MD.Efficacy of novel histone deacetylase inhibitor, AR42, in a mouse model of, human T-lymphotropic virus type 1 adult T cell lymphoma.Leuk Res. 2011 Nov;35(11):1491-7. Epub 2011 Jul 29.

[3]. Zhang S, Suvannasankha A, Crean CD, White VL, Chen CS, Farag SS.The novel histone deacetylase inhibitor, AR-42, inhibits gp130/Stat3 pathway and induces apoptosis and cell cycle arrest in multiple myeloma cells.Int J Cancer. 2011 Jul 1;129(1):204-13.

[4]. Lin TY et al. AR-42, a novel HDAC inhibitor, exhibits biologic activity against malignant mast cell lines via down-regulation of constitutively activated Kit. Blood. 2010 May 27;115(21):4217-25.

[5]. Shuhong Zhang et al. The novel histone deacetylase inhibitor, AR-42, inhibits gp130/Stat3 pathway and induces apoptosis and cell cycle arrest in multiple myeloma cells International Journal of Cancer Volume 129, Issue 1, pages 204-213, 1 July 2011

密度	1.223
分子式	C₁₈H₂₀N₂O₃
分子量	312.36300
精确质量	312.14700
PSA	78.43000
LogP	3.64780
外观性状	粉末
储存条件	-20℃

海关编码	2924299090

海关编码	2924299090
中文概述	2924299090. 其他环酰胺（包括环氨基甲酸酯）（包括其衍生物以及他们的盐）. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%
申报要素	品名, 成分含量, 用途, 包装
Summary	2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%