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编 号:F755546
分子式:C19H38ClNO2
分子量:347.96
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生物活性:
Antitumor agent-115 (SS-12) is an effective anti-tumor compound with an IC50 value of 0.34 μM-24.14 μM for cell line 4T1. Antitumor agent-115 can block the cell cycle of mouse breast cancer cell line 4T1, reduce the mitochondrial membrane potential, and induce apoptosis, and the IC50 value is 8-25 μmol/L for cell viability. Antitumor agent-115 can be used for breast cancer research.

体内研究:
Antitumor agent-115 (SS-12) (10 mg stachydrine/kg equivale, 200 μL, 口服给药) 在大鼠体内具有较高的生物利用度。 Antitumor agent-115 (0.1 mL/10 g, 口服给药) 在乳腺癌模型小鼠中具有抗肿瘤作用,并改善模型小鼠脾脏的形态结构。Animal Model:Rats
Dosage:10 mg stachydrine/kg equivale, 200 μL
Administration:Oral administration (p. o.)
Result:Exhibited high systemic exposure with 6.10 μg/mL of Cmax value and 14.75 h μg/mL of AUC0-tvalue.
Animal Model:Tumor-bearing mice
Dosage:0.2 mmol/kg
Administration:Oral administration (p. o.)
Result:Inhibitory rate was 51.47% ( P< 0.01)Displayed significant tumor cell shrinkage and larger void areas in tumor tissuesExhibited more weight loss than the model group and other treatment groups, increased of both AST and ALT levels and reduced spleen index of the tumor-bearing mice

体外研究:
Antitumor agent-115 (SS-12) (1.25 μM, 10 μm, 40 μM, 24 小时) 主要通过使细胞周期停滞在 G0/G1 阶段来诱导 4T1 细胞凋亡。Antitumor agent-115 (15 μM, 30 μM, 60 μM, 24小时) 抑制 4T1 细胞的迁移和侵袭。Antitumor agent-115 (10 μM, 24小时) 通过线粒体途径诱导 4T1 细胞凋亡。
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