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ENMD-1198

Catalog No. T15234 CAS 864668-87-1

Synonyms: 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

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

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Description	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.
In vitro	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].
In vivo	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].

Synonyms	IRC 110160, ENMD-119, ENMD 1198
Molecular Weight	311.42
Formula	C20H25NO2
CAS No.	864668-87-1

Storage

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

References and Literature

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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Keywords

ENMD-1198 864668-87-1 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells STAT HIF ENMD 119 ENMD119 IRC 110160 IRC-110160 IRC110160 ENMD-119 ENMD1198 ENMD 1198 inhibitor inhibit

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