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编 号：F391484
分子式：C15H12O6
分子量：288.25
分子式：C15H12O6
分子量：288.25
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CAS No: 56486-94-3
产品详情
生物活性：
Steppogenin is a potent inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. Steppogenin can be sued for the research of angiogenic diseases, such as those involving solid tumors.
体内研究：
Steppogenin (2 mg/kg，腹腔注射，一次) 抑制肿瘤生长和血管生成。Steppogenin (2 mg/kg，腹腔注射，一次) 在肝脏和脾脏中的分布最高 (分别为 25.5 倍和 9.74 倍 AUC 比率)，T1/2 显著更高。Pharmacokinetic Parameters of Steppogenin in male C57BL/6 J mice.Cmax (ng/mL) Tmax (h)T1/2 (h) AUC8h (ng/mL?h) AUC∞ (ng/mL?h) AUC ratio
Plasma448 ± 1130.250.49 ± 0.14283 ± 98.9284 ± 97.81
Tumor635 ± 1140.3 ± 0.11.87 ± 0.871078 ± 4941252 ± 5474.58
Liver4319 ± 10630.251.72 ± 0.266733 ± 13006967 ± 120025.5
Lung521 ± 1810.250.36 ± 0.12261 ± 96.1280 ± 1061.02
Heart285 ± 15.20.250.2107 ± 44.3176.90.65
Kidney1225 ± 4630.250.33 ± 0.01628 ± 234624.7 ± 2382.35
Spleen6110 ± 29540.250.47 ± 0.012443 ± 11552663 ± 12899.74
Brain309 ± 95.70.251.36 ± 0.46191 ± 67241 ± 75.40.88
Animal Model:C57BL/6 J mice (6-week-old, male, Lewis lung carcinoma (LLC) allograft tumor model)
Dosage:2 mg/kg
Administration:IP, once
Result:Significantly suppressed tumor growth.
Animal Model:C57BL/6 J mice (6-week-old, male, Lewis lung carcinoma (LLC) allograft tumor model)
Dosage:2 mg/kg
Administration:IP, once (Pharmacokinetic Analysis)
Result:Showed the highest distribution to the liver and spleen (25.5-fold and 9.74-fold AUC ratio, respectively) with significantly higher T1/2. may not be accumulated even in the highly distributed tissues after the repeated administration of steppogenin.
体外研究：
Steppogenin (0-10 μM, 24 h) 以剂量依赖性方式抑制 HEK293T 细胞缺氧条件下 HIF-1α 的转录活性和血管内皮细胞 (ECs) 中 VEGF 诱导的 DLL4 表达。Steppogenin (0-3 μM，6 h) 在缺氧条件下抑制 HIF-1α 靶基因（VEGF、GLUT1、CXCR4 和 CA9）的 mRNA 表达。Steppogenin (0-3 μM，16 h) 抑制 HIF-1α 蛋白水平，并抑制 VEGF、CXCR4 和 CA9 的蛋白水平。Steppogenin (0-3 μM，24 h) 抑制缺氧诱导的血管 EC 增殖和迁移以及 VEGF 诱导的 EC 球体发芽。
Steppogenin is a potent inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. Steppogenin can be sued for the research of angiogenic diseases, such as those involving solid tumors.
体内研究：
Steppogenin (2 mg/kg，腹腔注射，一次) 抑制肿瘤生长和血管生成。Steppogenin (2 mg/kg，腹腔注射，一次) 在肝脏和脾脏中的分布最高 (分别为 25.5 倍和 9.74 倍 AUC 比率)，T1/2 显著更高。Pharmacokinetic Parameters of Steppogenin in male C57BL/6 J mice.Cmax (ng/mL) Tmax (h)T1/2 (h) AUC8h (ng/mL?h) AUC∞ (ng/mL?h) AUC ratio
Plasma448 ± 1130.250.49 ± 0.14283 ± 98.9284 ± 97.81
Tumor635 ± 1140.3 ± 0.11.87 ± 0.871078 ± 4941252 ± 5474.58
Liver4319 ± 10630.251.72 ± 0.266733 ± 13006967 ± 120025.5
Lung521 ± 1810.250.36 ± 0.12261 ± 96.1280 ± 1061.02
Heart285 ± 15.20.250.2107 ± 44.3176.90.65
Kidney1225 ± 4630.250.33 ± 0.01628 ± 234624.7 ± 2382.35
Spleen6110 ± 29540.250.47 ± 0.012443 ± 11552663 ± 12899.74
Brain309 ± 95.70.251.36 ± 0.46191 ± 67241 ± 75.40.88
Animal Model:C57BL/6 J mice (6-week-old, male, Lewis lung carcinoma (LLC) allograft tumor model)
Dosage:2 mg/kg
Administration:IP, once
Result:Significantly suppressed tumor growth.
Animal Model:C57BL/6 J mice (6-week-old, male, Lewis lung carcinoma (LLC) allograft tumor model)
Dosage:2 mg/kg
Administration:IP, once (Pharmacokinetic Analysis)
Result:Showed the highest distribution to the liver and spleen (25.5-fold and 9.74-fold AUC ratio, respectively) with significantly higher T1/2. may not be accumulated even in the highly distributed tissues after the repeated administration of steppogenin.
体外研究：
Steppogenin (0-10 μM, 24 h) 以剂量依赖性方式抑制 HEK293T 细胞缺氧条件下 HIF-1α 的转录活性和血管内皮细胞 (ECs) 中 VEGF 诱导的 DLL4 表达。Steppogenin (0-3 μM，6 h) 在缺氧条件下抑制 HIF-1α 靶基因（VEGF、GLUT1、CXCR4 和 CA9）的 mRNA 表达。Steppogenin (0-3 μM，16 h) 抑制 HIF-1α 蛋白水平，并抑制 VEGF、CXCR4 和 CA9 的蛋白水平。Steppogenin (0-3 μM，24 h) 抑制缺氧诱导的血管 EC 增殖和迁移以及 VEGF 诱导的 EC 球体发芽。
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