1. Cytoskeleton
    Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. Microtubule/Tubulin
    HIF/HIF Prolyl-Hydroxylase
    STAT
  3. ENMD-1198

ENMD-1198 (Synonyms: IRC-110160)

Cat. No.: HY-16196 Purity: 98.87%
Handling Instructions

ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.

For research use only. We do not sell to patients.

ENMD-1198 Chemical Structure

ENMD-1198 Chemical Structure

CAS No. : 864668-87-1

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Estimated Time of Arrival: December 31
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Description

ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.

IC50 & Target[3]

STAT3

 

HIF-1α

 

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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).
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

311.42

Formula

C₂₀H₂₅NO₂

CAS No.
SMILES

C[[email protected]@]12C=CC[[email protected]@]1([H])[[email protected]]3([H])CCC4=C(C=C(OC)C(C(N)=O)=C4)[[email protected]@]3([H])CC2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
References
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Keywords:

ENMD-1198IRC-110160ENMD1198ENMD 1198IRC110160IRC 110160Microtubule/TubulinHIF/HIF Prolyl-HydroxylaseSTATHypoxia-inducible factorsHIFsHIF-PHhepatocellularcarcinomacellsHUH-7HepG2vascularizationInhibitorinhibitorinhibit

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ENMD-1198
Cat. No.:
HY-16196
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