| Identification | Back Directory | [Name]
(2R,4R)-4-Fluoro-1-[[1-(3-fluoro-4-methoxyphenyl)cyclohexyl]carbonyl]-N-1H-pyrazolo[4,3-b]pyridin-5-yl-2-pyrrolidinecarboxamide | [CAS]
2259641-24-0 | [Synonyms]
(2R,4R)-4-Fluoro-1-[[1-(3-fluoro-4-methoxyphenyl)cyclohexyl]carbonyl]-N-1H-pyrazolo[4,3-b]pyridin-5-yl-2-pyrrolidinecarboxamide | [Molecular Formula]
C25H27F2N5O3 | [MOL File]
2259641-24-0.mol | [Molecular Weight]
483.51 |
| Hazard Information | Back Directory | [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. |
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