ML00253764

Names

[ Name ]:
ML00253764

[Synonym ]:
1H-Imidazole, 2-[2-[2-(5-bromo-2-methoxyphenyl)ethyl]-3-fluorophenyl]-4,5-dihydro-, hydrochloride (1:1)
2-{2-[2-(5-Bromo-2-methoxyphenyl)ethyl]-3-fluorophenyl}-4,5-dihydro-1H-imidazole hydrochloride (1:1)
MFCD28133377

Biological Activity

[Description]:

ML00253764 is a selective melanocortin receptor 4 (MC4R) antagonist, can induce apoptosis by inhibiting ERK1/2 and Akt phosphorylation, and has anticancer activity[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> GPCR/G Protein >> Melanocortin Receptor

[In Vitro]

ML00253764(0.001-50 μM, 24 h or 72 h)对人胶质母细胞瘤细胞增殖具有显著的时间和浓度依赖性抑制活性，其中作用于 U-118 细胞的 IC50 值为 6.56 μM，可以诱导U-87细胞凋亡，且在这两种细胞系中均表现出显著的 ERK1/2 磷酸化抑制作用[1]。

[In Vivo]

ML00253764(30 mg/kg, s.c., daily, 34 days) 可抑制感染 U-87 细胞的 CD nu/nu 雄性小鼠肿瘤生长[1]。

[References]

[1]. Francesca Vaglini, et al. Melanocortin Receptor-4 and Glioblastoma Cells: Effects of the Selective Antagonist ML00253764 Alone and in Combination with Temozolomide In Vitro and In Vivo. Mol Neurobiol. 2018 Jun;55(6):4984-4997.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₈H₁₉BrClFN₂O

[ Molecular Weight ]:
413.712

[ Exact Mass ]:
412.035309

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.