681847-92-7

681847-92-7 structure

Name: ML00253764
Chemical Name: 2-{2-[2-(5-Bromo-2-methoxyphenyl)ethyl]-3-fluorophenyl}-4,5-dihydro-1H-imidazole hydrochloride (1:1)
CAS Number: 681847-92-7
Molecular Formula: C₁₈H₁₉BrClFN₂O
Molecular Weight: 413.712
Catalog: Research Areas Cancer
Create Date: 2018-06-12 03:44:53
Modify Date: 2024-01-08 02:34:31
ML00253764 is a selective melanocortin receptor 4 (MC4R) antagonist, can induce apoptosis by inhibiting ERK1/2 and Akt phosphorylation, and has anticancer activity[1].

Name	2-{2-[2-(5-Bromo-2-methoxyphenyl)ethyl]-3-fluorophenyl}-4,5-dihydro-1H-imidazole hydrochloride (1:1)
Synonyms	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

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.