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ML00253764

Names

[ CAS No. ]:
681847-92-7

[ 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