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编 号：F477330
分子式：C23H24N4O4
分子量：420.46
分子式：C23H24N4O4
分子量：420.46
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CAS No: 847460-34-8
产品详情
生物活性：
CRA-026440 is a potent, broad-spectrum HDAC inhibitor. The Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4, 14, 11, 15, 7, and 20 nM respectively. CRA-026440 shows antitumor and antiangiogenic activities. CRA-026440 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（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 对 HUVEC 内皮细胞具有抗增殖作用，GI50 值为 1.41 μM。CRA-026440（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（0.1-10 μM；5 天）以剂量依赖性方式抑制离体血管生成。
CRA-026440 is a potent, broad-spectrum HDAC inhibitor. The Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4, 14, 11, 15, 7, and 20 nM respectively. CRA-026440 shows antitumor and antiangiogenic activities. CRA-026440 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（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 对 HUVEC 内皮细胞具有抗增殖作用，GI50 值为 1.41 μM。CRA-026440（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（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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