产品
编 号:F363626
分子式:C26H34O6
分子量:442.54
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10mM*1mL in DMSO
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1mg
297
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2mg
505
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5mg
960
In-stock
10mg
1440
In-stock
50mg
3040
In-stock
100mg
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生物活性:
Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models.

体内研究:
Cinobufagin (腹腔注射 5 mg/kg,每天 1 次,持续 10 天) 在诱导肿瘤异种移植小鼠模型中通过抑制细胞凋亡来抑制异种移植物生长。Cinobufagin (腹腔注射 5 mg/kg,每天 1 次,持续 10 天) 抑制皮下和颅内 U87MG-EGFR 异种移植小鼠模型的肿瘤生长,并提高颅内携带 U87MGEGFR 肿瘤的裸鼠的中位生存率。Animal Model:OCM1 cells tumor xenograft in Nu/Nu nude mice
Dosage:5 mg/kg
Administration:Intraperitoneal injection (i.p.), once a day for 10 days
Result:Made the tumors grew more slowly than those treated with intraperitoneal injection of saline or untreated. Increased the expression of caspase-3 and PARP in tumor tissues and decreased Bcl-2 and Bcl-xl expression in mouse tumor tissues and increased expression of Bad and Bax.
Animal Model:U87MG-EGFR subcutaneous and intracranial xenograft model
Dosage:5 mg/kg
Administration:Intraperitoneal injection (i.p.), once a day for 10 days
Result:Decreased the luminescence intensity of brain tumor about 70%.Decreased p-EGFR, p-STAT3, and p-Akt levels in the intracranial tumors as compared with the vehicles.Decreased Ki67 and active caspase-3 immunostaining of intracranial tumors.

体外研究:
Conobafagin (30-300 nM,24 小时) 以浓度依赖性方式阻断细胞周期的 G1 期,并诱导 OCM1 细胞凋亡和凋亡相关蛋白的改变。 Conobufagin (30-300 nM,7 天) 在 葡萄膜黑色素瘤 OCM1 细胞中以剂量依赖的方式发挥有效的抗肿瘤活性。Conobafagin (0.01-1 μM,6 小时) 可阻断多形性胶质母细胞瘤 U87MG-EGFR 和 U87MG-PTEN 细胞中表皮生长因子受体 (EGFR) 磷酸化,诱导细胞凋亡和细胞毒性。Cinobufagin (0.4,0.7,1.0 μM,24-48 小时) 诱导细胞周期停滞在 G2/M 期并导致细胞凋亡,从而抑制黑色素瘤 A375/B16 细胞的增殖。
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