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ENMD-1198

产品编号 T15234 CAS 864668-87-1

别名: IRC 110160, ENMD-119, ENMD 1198

ENMD-119 is a 2-methoxyestradiol analog with antiproliferative and antiangiogenic activity. It is suitable for inhibiting HIF-1α and STAT3 in human HCC cells.

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ENMD-1198, CAS 864668-87-1

规格	价格/CNY	货期
25 mg	￥ 10,600	6-8周
50 mg	￥ 13,800	6-8周
100 mg	￥ 17,500	6-8周

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	ENMD-119 is a 2-methoxyestradiol analog with antiproliferative and antiangiogenic activity. It is suitable for inhibiting HIF-1α and STAT3 in human HCC cells.
体外活性	ENMD-1198 inhibits the proliferation of endothelial cell HMEC-1 and BMH29L (IC50: 0.4 μM and 3.8 μM) and it also significantly inhibits capillary tube formation from 0.1 μM and suppresses endothelial cell morphogenesis at 1 μM. ENMD-1198 inhibits endothelial cell motility and endothelial cell migration and inhibits MDA-BO2 cancer cell viability (IC50: approximately 0.8 μM). ENMD-1198 also inhibits the phosphorylation of MAPK/Erk, PI-3K/Akt, and FAK. ENMD-1198 (0.5 μM) inhibits the formation of capillary tubes in HMEC-1 cells. Moreover, ENMD-1198 at the IC50 for cell proliferation causes a significant decrease in VEGFR-2 expression both in the presence and in the absence of serum. ENMD-1198 rapidly causes extensive microtubule depolymerization and accumulation of actin stress fibers and large focal adhesions [1]. ENMD-1198 has both an antiangiogenic effect and a vascular disruptive effect in vitro. ENMD-1198 reduces the viability of RAW264.7 osteoclast precursor cells and inhibits PTHrP-stimulated bone resorption. ENMD-1198 shows inhibitory activity against RAW264 (IC50: approximately 0.4 μM) and is shown to be 4 times more potent than 2ME2 (IC50 appro 1.6 μM) [2]. The activation of HIF-1α and STAT3 is dramatically reduced by ENMD-1198, which leads to lower VEGF mRNA expression. In addition, the tumor cell migratory and invasive properties are obviously inhibited [3].
体内活性	ENMD-1198 treatment protects the bone against tumor-induced osteolysis in vivo [2]. ENMD-1198 (200 mg/kg/d, peroral gavage)-based combination treatments decrease tumor burden but do not eradicate the tumor in mice. ENMD-1198 (200 mg/kg/day, p.o.) leads to a significant reduction in tumor growth, tumor vascularization, and numbers of proliferating tumor cells [3].

别名	IRC 110160, ENMD-119, ENMD 1198
分子量	311.42
分子式	C20H25NO2
CAS No.	864668-87-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

计算器

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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.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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