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编 号:F750683
分子式:C25H27F2N5O3
分子量:483.51
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生物活性:
Ep300/CREBBP-IN-8 (Example 37) is a potent and orally active Ep300 and CREBBP inhibitor with IC50s of 0.014 and 0.018 μM, respectively. Ep300/CREBBP-IN-8 can be used for the research of cancer.

体内研究:
Ep300/CREBBP-IN-8 (Example 37; 6.25 mg/kg/day; oral; twice daily for 11 days) 抑制小鼠肿瘤增殖。Animal Model:Female BALB/c-nu/nu mice, LK2 cell subcutaneous transplant model
Dosage:6.25 mg/kg/day
Administration:Oral administration, twice a day for 11 days
Result:Inhibited tumor volume by 42%.

体外研究:
Ep300/CREBBP-IN-8 (Example 37) 抑制细胞内 H3K27Ac 活性,其 IC50 为 0.016 μM。Ep300/CREBBP-IN-8 (38 nM-10 mM; 3 days) 抑制 LK2 和 TE-8 细胞生长,GI50 分别为 85.917 μM 和 112.922 μM 。
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