864668-87-1
中文名稱
864668-87-1
英文名稱
ENMD-119
CAS
864668-87-1
分子式
C20H25NO2
分子量
311.42
MOL 文件
864668-87-1.mol
更新日期
2023/03/20 15:41:17
864668-87-1 結(jié)構(gòu)式
基本信息
中文別名
化合物 T15234 英文別名
ENMD-119ENMD 1198
IRC 110160
ENMD-119 (ENMD 1198)
Estra-1,3,5(10),16-tetraene-3-carboxamide, 2-methoxy-
常見問題列表
生物活性
ENMD-1198 (IRC-110160)，具有口服活性的微管 (microtubule) 靶向劑，是 2-methoxyestradiol 的類似物，具有抗腫瘤、抗血管生成功效，在人體 HCC 細(xì)胞中，ENMD-1198 抑制人肝癌細(xì)胞中的 HIF-1α 和 STAT3，并導(dǎo)致腫瘤生長和血管生成減少。靶點(diǎn)
|
STAT3
|
HIF-1α
|
體外研究
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). |
體內(nèi)研究
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. |