13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
在線訂購 免費訂購熱線：021-59541103 021-60443211
聯系人:高小姐
電話:021-59541103 021-60443211
手機:13585831301
Q Q： 3004967995
Email:3004967995@qq.com
詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 1mg 5mg 10mg 20mg |
| CAS | 864668-87-1 |
| 別名 | N/A |
| 化學名 | N/A |
| 分子式 | C20H25NO2 |
| 分子量 | 311.42 |
| 溶解度 | Soluble in DMSO |
| 儲存條件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述：
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.
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原創作者：上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
賬 號：2169 2341 6278
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