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ENMD-1198
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
ENMD-1198图片
CAS NO:864668-87-1
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议

产品名称
IRC-110160
产品介绍
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 activemicrotubule destabilizingagent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha andSTAT3in 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].

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].

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

性状

Solid

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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month