AbMole|AR-42（CAS号935881-37-1；目录号M3405）

AR-42是一种HDAC抑制剂，IC50为30 nM。AR-42 诱导细胞周期阻滞、凋亡和 caspases-3/7 活化。

生物活性

AR-42 is a novel HDAC inhibitor with an IC50 of 0.61 μM for acute lymphoblastic leukemia (697) cell lines. In chronic lymphocytic leukemia (CLL) cells, the 48-hr LC50 of AR-42  is 0.76 μM. AR-42 produces dose- and time-dependent acetylation both of histones and tubulin, and induces caspase-dependent apoptosis that is not reduced in the presence of stromal cells. AR-42  significantly reduced leukocyte counts and/or prolonged survival in three separate mouse models of B-cell malignancy without evidence of toxicity. AR-42 has in vitro and in vivo efficacy at tolerable doses. In additon, AR-42 promoted hyperacetylation of H3, H4, and alpha-tubulin, and up-regulation of p21. 

化学性质

分子量	312.36
分子式	C18H20N2O3
CAS号	935881-37-1
溶解性（25°C）	DMSO 20 mg/mL Ethanol 50 mg/mL
储存条件	粉末型式       -20°C   3年；4°C   2年 溶于溶剂       -80°C   6个月；-20°C   1个月
运输方式	冰袋运输，根据产品的不同，可能会有相应调整。

储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.2014 mL	16.0072 mL	32.0143 mL
5 mM	0.6403 mL	3.2014 mL	6.4029 mL
10 mM	0.3201 mL	1.6007 mL	3.2014 mL

参考文献

[1] D Bradley Welling, et al. Early phase clinical studies of AR-42, a histone deacetylase inhibitor, for neurofibromatosis type 2-associated vestibular schwannomas and meningiomas

[2] Ming Jang Chua, et al. Histone deacetylase inhibitor AR-42 and achiral analogues kill malaria parasites in vitro and in mice

[3] Sophia G Liva, et al. Phase I study of AR-42 and decitabine in acute myeloid leukemia

[4] Yuxuan Zhu, et al. AR-42: A Pan-HDAC Inhibitor with Antitumor and Antiangiogenic Activities in Esophageal Squamous Cell Carcinoma

[5] Mingming Zhang, et al. AR-42 induces apoptosis in human hepatocellular carcinoma cells via HDAC5 inhibition