(-)-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。
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.
性状
Solid
体外研究(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). has not independently confirmed the accuracy of these methods. They are for reference only.Cell Cycle Analysis
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. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (406.01 mM; Need ultrasonic)配制储备液