产品
编 号:F740996
分子式:C23H25ClN4O4
分子量:456.92
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1mg
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5mg
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10mg
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生物活性:
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. CRA-026440 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

体内研究:
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。Animal Model:HCT-116 tumor-bearing nude mice
Dosage:100 mg/kg
Administration:i.v.; daily; for three consecutive days
Result:Resulted in a statistically significant reduction in tumor growth.

体外研究:
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。
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