Ep300/CREBBP-IN-2

Names

[ CAS No. ]:
2259641-59-1

[ Name ]:
Ep300/CREBBP-IN-2

Biological Activity

[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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Epigenetics >> Histone Acetyltransferase

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C26H27F3N4O4

[ Molecular Weight ]:
516.51

Related Compounds