ENMD-1198

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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。

CAS NO:

864668-87-1

IRC-110160

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°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month