Uses
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].
in vivo
Ep300/CREBBP-IN-8 (Example 37; 6.25 mg/kg/day; oral; twice daily for 11 days) inhibits tumor proliferation in mice[1].
| Animal Model: | Female BALB/c-nu/nu mice, LK2 cell subcutaneous transplant model[1] |
| Dosage: | 6.25 mg/kg/day |
| Administration: | Oral administration, twice a day for 11 days |
| Result: | Inhibited tumor volume by 42%. |
IC 50
EP300: 0.014 μM (IC50); CREBBP: 0.018 μM (IC50)
References
[1] NAITO Hiroyuki, et al. EP300 / CREBBP inhibitor. Patent JPWO2018235966A1.
