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。
| 生物活性 |
ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization. |
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| 体外研究 |
ENMD-1198 (0-5 μM; 24 hours) leads to a significant dose-dependent inhibition of HCC cell growth with IC50s of 2.5 μM for HUH-7 and HepG2 cells, respectively. Cell Viability Assay
Western Blot Analysis
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| 体内研究 |
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.
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| 分子式 |
C20H25NO2
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| 分子量 |
311.42
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| CAS号 |
864668-87-1
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
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纯度： 98%
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