ENMD-1198

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.In VitroENMD-1198 (0-5 μM; 24 hours) leads to a significant dose-dependent inhibition of HCC cell growth with IC 50 s of 2.5 μM for HUH-7 and HepG2 cells, respectively. 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). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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 AnalysisCell 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 VivoENMD-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. 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)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.Form:Solid. Molecular Formula: C20H25NO2. Molecular Weight: 311.42. PubChem CID: 11483754. Isomeric SMILES: C[C@]12CC[C@H]3[C@H]([C@@H]1CC=C2)CCC4=CC(=C(C=C34)OC)C(=O)N.