2259641-59-1
2259641-59-1 structure
- Name: Ep300/CREBBP-IN-2
- Chemical Name: Ep300/CREBBP-IN-2
- CAS Number: 2259641-59-1
- Molecular Formula: C26H27F3N4O4
- Molecular Weight: 516.51
- Catalog: Signaling Pathways Epigenetics Histone Acetyltransferase
- Create Date: 2023-05-31 19:56:15
- Modify Date: 2024-04-09 16:39:56
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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[1].
| Name | Ep300/CREBBP-IN-2 |
|---|
| Description | 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[1]. |
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| Related Catalog | |
| Target |
EP300:0.052 μM (IC50) CREBBP:0.148 μM (IC50) |
| In Vitro | Ep300/CREBBP-IN-2 (Example 73) 抑制细胞内 H3K27Ac 活性，其 IC50 为 0.070 μM[1]。 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 [1]。 Cell Viability Assay[1] Cell Line: LK2 and TE-8 cells Concentration: 38 nM-10 mM Incubation Time: 3 days Result: Inhibited LK2 and TE-8 cell growth with GI50s of 610.15 and 619.505 μM, respectively. |
| In Vivo | Ep300/CREBBP-IN-2 (Example 73; 2 mg/kg/day; oral; twice daily for 9 days) 抑制小鼠肿瘤增殖[1]。 Animal Model: Female BALB/c-nu/nu mice, TE-8 cell subcutaneous transplant model[1] Dosage: 2 mg/kg/day Administration: Oral administration, twice a day for 9 days Result: Inhibited tumor volume by 65%. |
| References |
[1]. NAITO Hiroyuki, et al. EP300 / CREBBP inhibitor. Patent JPWO2018235966A1. |
| Molecular Formula | C26H27F3N4O4 |
|---|---|
| Molecular Weight | 516.51 |