产品
编 号:F756993
分子式:C24H29ClN2O4
分子量:444.95
产品类型
结构图
CAS No: 2927489-95-8
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产品详情
生物活性:
MAO A/HSP90-IN-1 (4-b) is a MAO A/HSP90 dual inhibitor with IC50 value of 1.77 μM and 0.019 μM in Glioblastoma (GBM) GL26 cells and HSP90α, respectively. MAO A/HSP90-IN-1 (4-b) can inhibit MAO A activity, HSP90 binding and the expression of HER2 and phospho-Akt to inhibit the growth of GBM, they also reduce PD-L1 expression, which inhibits T cell activation. MAO A/HSP90-IN-1 (4-b) have potential to inhibit tumor immune escape. MAO A/HSP90-IN-1 (4-b) can be used for brain tumor-related diseases research.
体内研究:
MAO A/HSP90-IN-1 (4-b) (25 mg/kg,腹腔注射,每天) 抑制 GBM 小鼠模型肿瘤生长。Animal Model:GL26 GBM mouse model
Dosage:25 mg/kg
Administration:Intraperitoneal injection (i.p.)
Result:Decreased tumor growth inhibition (TGI%) was 63.2% compared to vehicle group.
体外研究:
MAO A/HSP90-IN-1 (4-b) (0.1 μM-3 μM, 24小时) 通过抑制 MAO A 和 HSP90,从而减少 GBM 细胞的增殖。MAO A/HSP90-IN-1 (0.1 μM-3 μM, 24小时) 在 GL26 中的 IC50 为0.73 μM,在GL26中的 IC50 为1.68 μM,在 U251R 中的 IC50 为0.84 μM。MAO A/HSP90-IN-1 (0μM, 0.35μM, 0.7μM, 1.4μM, 24小时) 在小鼠胶质瘤 GL26 细胞中抑制IFN-γ 诱导的PD-L1表达。