CRA-026440 hydrochloride 是一种有效的广谱HDAC(HDAC) 抑制剂。作用于HDAC1，HDAC2，HDAC3，HDAC6，HDAC8和HDAC10的Ki分别为 4 nM，14 nM，11 nM，15 nM，7 nM 和 20 nM。CRA-026440 hydrochloride 具有抗肿瘤和抗血管生成活性。
| 生物活性 | CRA-026440 hydrochloride is a potent, broad-spectrumHDAC(HDAC) inhibitor. TheKivalues against recombinantHDACisoenzymesHDAC1,HDAC2,HDAC3,HDAC6,HDAC8, andHDAC10are 4 nM, 14 nM, 11 nM, 15 nM, 7 nM, and 20 nM respectively. CRA-026440 hydrochloride shows antitumor and antiangiogenic activities[1]. |
| IC50& Target[1] | HDAC1 4 nM (IC50) | HDAC2 14 nM (IC50) | HDAC3/SMRT 11 nM (IC50) | HDAC6 15 nM (IC50) | HDAC8 7 nM (IC50) | HDAC10 20 nM (IC50) |
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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[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. |
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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[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. |
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| 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 | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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