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编 号:F762932
分子式:C21H30Br3ClN6S
分子量:673.73
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生物活性:
SIRT6-IN-3 (compound 8a) is a selective inhibitor of SIRT6 (IC50=7.49 μM). SIRT6-IN-3 inhibits pancreatic ductal adenocarcinoma (PDAC) cells proliferation and induces apoptosis. SIRT6-IN-3 increases the sensitivity of cancer cells to gemcitabine (HY-17026) via blocking the DNA damage repair pathway. SIRT6-IN-3 is used in pancreatic cancer research.

体内研究:
SIRT6-IN-3 (HY-156027;20 mg/kg,腹腔注射;两天一次,连用四周) 在肿瘤小鼠模型中有抗肿瘤作用。SIRT6-IN-3 (HY-156027;20 mg/kg,腹腔注射;两天一次,连用四周) 在与吉西他滨 (比例 2 : 1 ) 联用时增强了吉西他滨的抗肿瘤作用。Animal Model:Tumor mouse model
Dosage:20 mg/kg (in combination with 10 mg/kg gemcitabine)
Administration:Intraperitoneal injection (i.p.); Once every 2 days for 4 weeks
Result:Inhibited the tumor mass 71.3% in mice with combinations of gemcitabine.Greatly increased the expression of apoptosis maker.

体外研究:
SIRT6-IN-3 (25 μM,48 小时) 诱导 PDAC 细胞周期阻滞和细胞凋亡。SIRT6-IN-3 (25 μM,72 小时) 通过抑制细胞信号通路来抑制胰腺癌细胞的增殖。
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