(-)-Irofulven

(-)-Irofulven (MGI 114), an Illudin S analog, is a DNA alkylating agent. (-)-Irofulven inhibits the replication of DNA, induces tumor cells apoptosis , and has potent antitumor activity.In Vitro(-)-Irofulven (2.8 μM; 1 hour) induces p53-dependent cell cycle arrest. (-)-Irofulven (0.8 μM, 0.9 μM and 2.8 μM; 1 hour) induces CHK2 activation is related to p53 status in cells. (-)-Irofulven inhibits DNA replication and induces chromosome aberrations (breaks and radials). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cycle AnalysisCell Line: A2780, CAOV3 and HCT116 cells Concentration: 2.8 μM Incubation Time: 1 hour Result: p53 wild-type cells mainly arrested at G1/S phases, while p53-mutated or p53- cells arrested at S and G2/M phases. Western Blot AnalysisCell Line: A2780, CAOV3 and HCT116 cells Concentration: 0.8 μM, 0.9 μM and 2.8 μM Incubation Time: 1 hour Result: Induced the Thr 68 phosphorylation of CHK2 kinase in cells.In Vivo(-)-Irofulven (7 mg/kg; i.p; on days 1-5 and 8-12) produces a statistically significant increase in the median survival of mice bearing tumor cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male and female athymic BALB/c mice (nu/nu genotype, 6 weeks old or older) injected with human glioblastoma multiforme. Dosage: 7 mg/kg Administration: i.p; on days 1-5 and 8-12 Result: Was active against all tumor lines.Form:Solid. Specification: 0.98 Molecular Formula: C15H18O3 Molecular Weight: 246.3 PubChem CID: 148189 Isomeric SMILES: CC1=C(C2=C(C3(CC3)[C@@](C(=O)C2=C1)(C)O)C)CO