(-)-Irofulven(Synonyms: MGI 114; 6-Hydroxymethylacylfulvene; NSC 683863)

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(-)-Irofulven (Synonyms: MGI 114; 6-Hydroxymethylacylfulvene; NSC 683863)

(-)-Irofulven (MGI 114) 是一种 Illudin S 类似物，是一种 DNA 烷化剂。(-)-Irofulven 抑制 DNA 复制，诱导肿瘤细胞凋亡 (apoptosis)，并具有有效的抗肿瘤活性。

(-)-Irofulven(Synonyms: MGI 114; 6-Hydroxymethylacylfulvene; NSC 683863)

(-)-Irofulven Chemical Structure

CAS No. : 158440-71-2

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生物活性

(-)-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[1][2].

体外研究
(In Vitro)

(-)-Irofulven (2.8 μM; 1 hour) induces p53-dependent cell cycle arrest[1].
(-)-Irofulven (0.8 μM, 0.9 μM and 2.8 μM; 1 hour) induces CHK2 activation is related to p53 status in cells[1].
(-)-Irofulven inhibits DNA replication and induces chromosome aberrations (breaks and radials)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell 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-null cells arrested at S and G2/M phases.

Western Blot Analysis[1]

Cell 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.

体内研究
(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[2].

上海金畔生物科技有限公司 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[2].
Dosage: 7 mg/kg
Administration: i.p; on days 1-5 and 8-12
Result: Was active against all tumor lines.

分子量

246.30

Formula

C15H18O3
CAS 号

158440-71-2
中文名称

(-)-伊洛福芬；伊罗夫文；6-羟甲基环二烯
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Yutian Wang, et al. Irofulven induces replication-dependent CHK2 activation related to p53 status. Biochem Pharmacol. 2007 Feb 15;73(4):469-80.

    [2]. H S Friedman, et al. Activity of irofulven (6-hydroxymethylacylfulvene) in the treatment of glioblastoma multiforme-derived xenografts in athymic mice. Cancer Chemother Pharmacol. 2001 Nov;48(5):413-6.

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