Bioactivity | 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[1]. |
Invitro | Ep300/CREBBP-IN-8 (Example 37) 抑制细胞内 H3K27Ac 活性,其 IC50 为 0.016 μM[1]。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 [1]。 Cell Viability Assay[1] Cell Line: |
In Vivo | 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[1]。 Animal Model: |
Name | Ep300/CREBBP-IN-8 |
CAS | 2259641-24-0 |
Formula | C25H27F2N5O3 |
Molar Mass | 483.51 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. NAITO Hiroyuki, et al. EP300 / CREBBP inhibitor. Patent JPWO2018235966A1. |