CRA-026440 hydrochloride is a potent, broad-spectrum HDAC (HDAC) inhibitor. The Ki 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[1].
CRA-026440 hydrochloride 对 HUVEC 内皮细胞具有抗增殖作用，GI50 值为 1.41 μM[1]。
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[1]。
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[1]。
Western Blot Analysis[1]
| Cell Line: | HCT116 cells |
| Concentration: | 0.1 μM, 0.5 μM, 1 μM, 5 μM, 10 μM |
| Incubation Time: | 18 hours |
| Result: | Resulted in the accumulation of both acetylated histones and acetylated tubulin. Induced expression of the cyclin-dependent kinase inhibitor p21Cip1/WAF1. |
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[1]。
| Animal Model: | HCT-116 tumor-bearing nude mice[1] |
| Dosage: | 100 mg/kg |
| Administration: | i.v.; daily; for three consecutive days |
| Result: | Resulted in a statistically significant reduction in tumor growth. |
[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.