| Bioactivity | ML00253764 is a selective melanocortin receptor 4 (MC4R) antagonist, can induce apoptosis by inhibiting ERK1/2 and Akt phosphorylation, and has anticancer activity[1]. | ||||||||||||
| Invitro | 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]。 | ||||||||||||
| Name | ML00253764 | ||||||||||||
| CAS | 681847-92-7 | ||||||||||||
| Formula | C18H18BrFN2O | ||||||||||||
| Molar Mass | 377.25 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [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. |
ML00253764
CAS: 681847-92-7 F: C18H18BrFN2O W: 377.25
ML00253764 is a selective melanocortin receptor 4 (MC4R) antagonist, can induce apoptosis by inhibiting ERK1/2 and Akt p
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