864668-87-1
| 中文名称 | 864668-87-1 |
|---|---|
| 中文同义词 | 化合物 T15234;化合物 ENMD-1198 |
| 英文名称 | ENMD-119 |
| 英文同义词 | ENMD-119;ENMD 1198;IRC 110160;ENMD-119 (ENMD 1198);Estra-1,3,5(10),16-tetraene-3-carboxamide, 2-methoxy- |
| CAS号 | 864668-87-1 |
| 分子式 | C20H25NO2 |
| 分子量 | 311.42 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 864668-87-1.mol |
| 结构式 |  |
864668-87-1 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 固体 |
| 颜色 | 白色至黄色 |
ENMD-1198 (IRC-110160)，具有口服活性的微管 (microtubule) 靶向剂，是 2-methoxyestradiol 的类似物，具有抗肿瘤、抗血管生成功效，在人体 HCC 细胞中，ENMD-1198 抑制人肝癌细胞中的 HIF-1α 和 STAT3，并导致肿瘤生长和血管生成减少。
|
STAT3
|
HIF-1α
|
ENMD-1198 (0-5 μM; 24 hours) leads to a significant dose-dependent inhibition of HCC cell growth with IC
50
s of 2.5 μM for HUH-7 and HepG2 cells, respectively.
ENMD-1198 (2.5 μM; 16 hours) abrogates EGF-induced phosphorylation of Akt (HUH-7), FAK (HUH-7), p44/42 MAPK (HepG2), and STAT3 (HUH-7, HepG2).
Cell Viability Assay
| Cell Line: | HUH-7 and HepG2 cells |
| Concentration: | 0-5 μM |
| Incubation Time: | 24 hours |
| Result: | Led to a significant dose-dependent inhibition of HCC cell growth. |
Western Blot Analysis
| Cell Line: | HUH-7 and HepG2 cells |
| Concentration: | 2.5 μM |
| Incubation Time: | 16 hours |
| Result: | Abrogated EGF-induced phosphorylation of Akt (HUH-7), FAK (HUH-7), p44/42 MAPK (HepG2), and STAT3 (HUH-7, HepG2). |
ENMD-1198 (200 mg/kg; p.o.; daily from day 7 to day 19) effectively inhibits growth of hepatocellular carcinoma through direct effects on the tumor cells, and also through inhibition of angiogenesis.
| Animal Model: | Eight-week-old male athymic nude mice (BALB/c nu/nu) (xenografted hepatocellular tumors) |
| Dosage: | 200 mg/kg |
| Administration: | P.o.; daily from day 7 to day 19 |
| Result: | Led to a significant growth inhibition of xenografted hepatocellular tumors. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-16196 | 864668-87-1 ENMD-1198 | 864668-87-1 | 1mg | 5000元 |
| 2024/08/19 | HY-16196 | ENMD-1198 | 10 mM * 1 mLin DMSO | 17128元 |