(-)-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
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(-)-Irofulven
CAS number：158440-71-2 molecular formula：C15H18O3
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| Chinese alias | (-)-艾洛福文 | ||
| English alias | Irofulven | IROFULVEN [WHO-DD] | DB05786 | Spectrum5_001233 | 6-Hydroxymethylacylfulvene | MGI 114 | NICJCIQSJJKZAH-AWEZNQCLSA-N | HMAF | BDBM50410835 | Urox ha | MGI.114 | 6-(Hydroxymethyl)acylfulvene | 6B799IH05A | Irofulven [USAN:INN] | apomorphine-hcl | ||
| CAS number | 158440-71-2 | molecular formula | C15H18O3 |
| molecular weight | 246.3 g/mol | Exact mass | ≥98% |
| PSA | 57.500 Ų | logp | -0.2 |
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