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编 号:F749545
分子式:C18H23NO4
分子量:317.38
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生物活性:
SPC-180002 is a SIRT1/3 dual inhibitor, with IC50 values of 1.13 and 5.41 μM, respectively. SPC-180002 disturbs redox homeostasis via ROS generation, which leads to an increase in both p21 protein stability and mitochondrial dysfunction. SPC-180002 strongly inhibits cell cycle progression and cancer cell growth. SPC-180002 activates the Nrf2 signaling pathway.

体内研究:
SPC-180002(1-5mg/kg,每周两次,腹腔注射)可抑制多种癌细胞的生长,并阻碍 MCF7 肿瘤异种移植小鼠中的肿瘤生长。Animal Model:Five weeks female athymic nude mice (BALB/c)
Dosage:1 mg/kg or 5 mg/kg
Administration:i.p., twice a week
Result:Significantly impeded tumor progression. The gain of tumor volume in SPC-180002-treated mice was significantly reduced by 48% at the low dose (1 mg/kg) and by 52% at the high dose (5 mg/kg), compared to vehicle-treated mice.

体外研究:
SPC-180002(0-5 μM,24 小时)通过 p21 积累抑制细胞周期进程,从而导致随后的细胞衰老。SPC-180002 不会诱导细胞凋亡和自噬。
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