产品
编 号:F750687
分子式:C26H27F3N4O4
分子量:516.51
产品类型
结构图
CAS No: 2259641-59-1
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产品详情
生物活性:
Ep300/CREBBP-IN-2 (Example 73) is a potent and orally active Ep300 and CREBBP inhibitor with IC50s of 0.052 and 0.148 μM, respectively. Ep300/CREBBP-IN-2 can be used for the research of cancer.
体内研究:
Ep300/CREBBP-IN-2 (Example 73; 2 mg/kg/day; oral; twice daily for 9 days) 抑制小鼠肿瘤增殖。Animal Model:Female BALB/c-nu/nu mice, TE-8 cell subcutaneous transplant model
Dosage:2 mg/kg/day
Administration:Oral administration, twice a day for 9 days
Result:Inhibited tumor volume by 65%.
体外研究:
Ep300/CREBBP-IN-2 (Example 73) 抑制细胞内 H3K27Ac 活性,其 IC50 为 0.070 μM。Ep300/CREBBP-IN-2 (38 nM-10 mM; 3 days) 抑制 LK2 和 TE-8 细胞生长,GI50 分别为 610.15 μM 和 619.505 μM 。