ENMD-119 (ENMD 1198)
(Synonyms: IRC-110160) 目录号 : GC33170
ENMD-119 (ENMD 1198) (IRC-110160) 是一种口服活性微管去稳定剂，是一种具有抗增殖和抗血管生成活性的 2-甲氧基雌二醇类似物。 ENMD-119 (ENMD 1198) 适用于抑制人类 HCC 细胞中的 HIF-1alpha 和 STAT3，并导致肿瘤生长和血管形成减少。
Cas No.:864668-87-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | To evaluate cytotoxic effects of ENMD-1198 on tumor cells, HUH-7 and HepG2 cells are seeded into 96-well plates (1×103/well; 12 wells per condition) and exposed to various concentrations of ENMD-1198 for 24 and 48 hours at 37°C. Methylthiazole tetrazolium (MTT) assay is used to assess cell proliferation. |
Animal experiment: | In brief, 2 holes are drilled through the bone cortex of the upper right tibia with a 25-gauge needle (25G 5/8) and bone marrow is flushed out. Subsequently, 250,000 MDA-BO2 cells/10 μL PBS is injected into the right tibiae of 6-week-old nude mice. Three days after intraosseous inoculation of MDA-BO2 cells, the animals are randomly divided in groups (n = 10). In a first experiment, 4 groups of mice (n = 10) receive either ENMD-1198 (200 mg/kg/d, per oral gavage) or CTX (30 mg/kg/d, through the drinking water) or a combination of ENMD-1198 and CTX or vehicle control. Treatment starts at day 7 after inoculation and is continued throughout the experiment. After 6 weeks, the animals are sacrificed by cervical dislocation and hindlimbs are fixed and kept for ex vivo X-ray analysis. In a second experiment, 4 groups of mice (n = 10) receive ENMD-1198 (200 mg/kg/d, per oral gavage) or ENMD-1198 + CTX (30 mg/kg/d, through the drinking water) or ENMD-1198 + CTX + risedronic acid (1.6 μmol/kg/d, by subcutaneous injection). |
References: [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. | |
ENMD-119 is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity, and is suitable for inhibiting HIF-1α and STAT3 in human HCC cells.
ENMD-1198 inhibits the proliferation of endothelial cell HMEC-1 and BMH29L with IC50 of 0.4 μM and 3.8 μM, respectively. ENMD-1198 (0.5 μM) inhibits the formation of capillary tubes in HMEC-1 cells. ENMD-1198 also significantly inhibits capillary tube formation from 0.1 μM and suppresses endothelial cell morphogenesis at 1 μM. 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 inhibits endothelial cell motility, ENMD-1198 inhibits endothelial cell migration. ENMD-1198 rapidly induces extensive microtubule depolymerization and accumulation of actin stress fibers and large focal adhesions[1]. ENMD-1198 inhibits MDA-BO2 cancer cell viability with an IC50 of approximately 0.8 μM. 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 with an IC50 value of approximately 0.4 μM and is shown to be 4 times more potent than 2ME2 (IC50 appro 1.6 μM)[2]. ENMD-1198 inhibits the phosphorylation of MAPK/Erk, PI-3K/Akt and FAK. Moreover, activation of HIF-1α and STAT3 is dramatically reduced by ENMD-1198, which results in lower VEGF mRNA expression. In addition, tumor cell migratory and invasive properties are significantly inhibited[3].
ENMD-1198 (200 mg/kg/d, per oral gavage)-based combination treatments reduce tumor burden but does not eradicate the tumor in mice. ENMD-1198 treatment protects the bone against tumor-induced osteolysis in vivo[2]. 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].
[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.
| Cas No. | 864668-87-1 | SDF | |
| 别名 | IRC-110160 | ||
| Canonical SMILES | C[C@@]12C=CC[C@@]1([H])[C@]3([H])CCC4=C(C=C(OC)C(C(N)=O)=C4)[C@@]3([H])CC2 | ||
| 分子式 | C20H25NO2 | 分子量 | 311.42 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2111 mL | 16.0555 mL | 32.111 mL |
| 5 mM | 0.6422 mL | 3.2111 mL | 6.4222 mL |
| 10 mM | 0.3211 mL | 1.6055 mL | 3.2111 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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