CRA-026440 hydrochloride is a potent, broad-spectrum HDAC (HDAC) inhibitor. The K i values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4 nM, 14 nM, 11 nM, 15 nM, 7 nM, and 20 nM respectively. CRA-026440 hydrochloride shows antitumor and antiangiogenic activities.
性状
Solid
IC50 & Target[1][2]
HDAC1 4 nM (IC50) HDAC2 14 nM (IC50
体外研究(In Vitro)
CRA-026440 hydrochloride 对 HUVEC 内皮细胞具有抗增殖作用,GI50 值为 1.41 μM。CRA-026440 hydrochloride(0.1-10 μM;18 小时)导致乙酰化组蛋白和乙酰化微管蛋白的积累,从而抑制肿瘤细胞生长并诱导细胞凋亡。CRA-026440 hydrochloride(0.1-10 μM;5 天)以剂量依赖性方式抑制离体血管生成。 has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis
体内研究(In Vivo)
CRA-026440 hydrochloride(100 mg/kg;静脉注射;每天;连续三天)导致携带 HCT116 或 U937 人肿瘤异种移植物的小鼠肿瘤生长显着减少。 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: HCT-116 tumor-bearing nude mice
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
参考文献
[1]. [1]Cao ZA, et al. CRA-026440: a potent, broad-spectrum, hydroxamic histone deacetylase inhibitor with antiproliferative and antiangiogenic activity in vitro and in vivo. Mol Cancer Ther. 2006 Jul;5(7):1693-701.