中文名 | 魚藤素 |
英文名 | DEGUELIN |
别名 | 藤素 魚藤素 AKT抑制剂(DEGUELIN) |
英文别名 | DEGUELIN (-)-Deguelin (-)-DEGUELIN (7as-cis)-oxy- (7aS,13aS)-13,13a-Dihydro-9,10-dimethoxy-3,3-dimethyl-(3H)-bis[1]benzopyrano[3.4-b.6'.5'-e]pyran-7(7aH)-one |
CAS | 522-17-8 |
EINECS | 200-258-5 |
化学式 | C23H22O6 |
分子量 | 394.42 |
密度 | 1?+-.0.06 g/cm3(Predicted) |
熔点 | 85-87°C(lit.) |
沸点 | 560.1±50.0 °C(Predicted) |
比旋光度 | D27 -97.2° (c = 0.2 in benzene) |
溶解度 | DMSO: >10 mg/mL |
存储条件 | -20°C |
稳定性 | 从提供的购买之日起稳定2年。在DMSO或乙醇中的溶液可以在-20 ° 储存长达3个月。 |
外观 | 固体 |
颜色 | white to yellow |
物化性质 | 生物活性 Deguelin 是一种天然存在的鱼藤酮类化合物,通过阻止多种途径 (如 PI3K-Akt,IKK-NF-κB 和 MAPK-mTOR-survivin 等) 充当化学预防剂。Deguelin 与 Hsp90 的结合导致许多致癌蛋白 (包括 MEK1/2,Akt,HIF1α,COX-2 和 NF-κB) 的表达降低。 |
MDL号 | MFCD01740600 |
体外研究 | Deguelin (0-500 nM) in a dose and time dependent manner inhibits the growth of MDA-MB-231, MDA-MB-468, BT-549 and BT-20 cells. Deguelin at all concentrations fails to reduce cell numbers in the presence of 1 ng EGF but in the presence of EGF 20 ng reinstated deguelin mediated growth inhibition. Deguelin treated cells show reduced expression of Survivin as determined by western blot and immunofluorescence examinations. Deguelin inhibits p-ERK and its downstream target p-STAT-3 and c-Myc expression in a dose dependent manner. Deguelin down-regulates Akt signaling probably by disrupting its association with Hsp 90 in cultured HNSCC cells. Deguelin deguelin disrupts the association between Hsp 90 with survivin and Cdk4. Deguelin deguelin treatment increases cellular ceramide level through de novo synthase pathway to mediate HNSCC cell death and apoptosis. Deguelin inhibits the proliferation of MPC-11 cells in a concentration- and time-dependent manner and causes the apoptotic death of MPC-11 cells. Following exposure to deguelin, the phosphorylation of Akt is decreased. Deguelin-induced apoptosis is characterized by the upregulation of Bax, downregulation of Bcl-2 and activation of caspase-3. |
体内研究 | Deguelin (2 or 4 mg/kg, i.p.) reduces the in vivo tumor growth of MDA-MB-231 cells transplanted subcutaneously in athymic mice. Deguelin (4 mg/kg, p.o.) treatment shows a great inhibition in tumor growth, which is demonstrated by reduced tumor size and improved mice survival and, indicating a significant anti-tumor ability by deguelin in vivo. In the colon cancer xenograft model, the volume of the tumor treated with deguelin is significantly lower than that of the control, and the apoptotic index for deguelin-treated mice is much higher. |
安全术语 | S22 - 切勿吸入粉尘。 S24/25 - 避免与皮肤和眼睛接触。 |
WGK Germany | 3 |
RTECS | DX1500000 |
海关编号 | 29329990 |
微信搜索化工百科或扫描下方二维码,添加化工百科小程序,随时随地查信息!