ENMD-1198(Synonyms: IRC-110160)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ENMD-1198 (Synonyms: IRC-110160) 纯度: 98.87%

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。

ENMD-1198(Synonyms: IRC-110160)

ENMD-1198 Chemical Structure

CAS No. : 864668-87-1

规格 价格 是否有货 数量
1 mg ￥5000 In-stock
5 mg   询价  
10 mg   询价  

* Please select Quantity before adding items.

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.

IC50 & Target[3]

STAT3

 

HIF-1α

 

体外研究
(In Vitro)

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[3].
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)[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[3]

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[3]

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).

体内研究
(In Vivo)

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[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Eight-week-old male athymic nude mice (BALB/c nu/nu) (xenografted hepatocellular tumors)[3]
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.

分子量

311.42

Formula

C20H25NO2
CAS 号

864668-87-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Pasquier E, et al. ENMD-1198, a new analogue of 2-methoxyestradiol, displays both antiangiogenic and vascular-disrupting properties. Mol Cancer Ther. 2010 May;9(5):1408-18.

    [2]. Snoeks TJ, et al. 2-methoxyestradiol analogue ENMD-1198 reduces breast cancer-induced osteolysis and tumor burden both in vitro and in vivo. Mol Cancer Ther. 2011 May;10(5):874-82.

    [3]. Moser C, et al. ENMD-1198, a novel tubulin-binding agent reduces HIF-1alpha and STAT3 activity in human hepatocellular carcinoma(HCC) cells, and inhibits growth and vascularization in vivo. BMC Cancer. 2008 Jul 23;8:206.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务