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生物来源
synthetic (organic)
质量水平
检测方案
≥95%
形式
powder or flakes
solid
溶解性
DMSO: 4 mg/mL
储存温度
−20°C
SMILES字符串
C[C@@H]([C@@H](C)N1CC(=O)NC(=O)C1)N2CC(=O)NC(=O)C2
InChI
1S/C12H18N4O4/c1-7(15-3-9(17)13-10(18)4-15)8(2)16-5-11(19)14-12(20)6-16/h7-8H,3-6H2,1-2H3,(H,13,17,18)(H,14,19,20)/t7-,8+
InChI key
OBYGAPWKTPDTAS-OCAPTIKFSA-N
一般描述
ICRF-193是一种双二哌嗪衍生物。它通过形成不可裂解的复合物来抑制拓扑异构酶II。
应用
ICRF-193已被用作拓扑异构酶II（TOP2）抑制剂，用于处理小鼠卵母细胞，以研究TOP2在减数分裂中的作用。
生化/生理作用
ICRF-193有助于增强细胞周期而不会导致无染色体分离。 它被认为是急性早幼粒细胞白血病（APL）的重要化学分化治疗药物。ICRF-193可用作抗癌药之间的分化诱导剂。
ICRF-193诱导一个G2检查点，该检查点与ATR依赖性的polo样激酶1（plk1）活性抑制和细胞周期蛋白B1磷酸化水平降低有关。 诱导K562和Molt-4等多种细胞系的凋亡。 ICRF-193是拓扑异构酶II抑制剂，对拓扑异构酶II-β比拓扑异构酶II-α更有效，可能还会导致DNA链断裂。
警示用语：
Danger
危险声明
危险分类
Acute Tox. 3 Oral - Skin Sens. 1
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
K Iguchi et al.
Biochemical pharmacology, 57(10), 1105-1111 (2001-03-07)
As many antitumor drugs can kill tumors through the induction of apoptosis, the effect of these drugs presumably would be enhanced if they were used in combination with other drugs that interact with apoptotic processes. To clarify the biological events
The catalytic DNA topoisomerase II inhibitor ICRF-193 and all-trans retinoic acid cooperatively induce granulocytic differentiation of acute promyelocytic leukemia cells: candidate drugs for chemo-differentiation therapy against acute promyelocytic leukemia
Niitsu,
Experimental Hematology, 30(11), 1273-1282 (2002)
DNA topoisomerase II is dispensable for oocyte meiotic resumption but is essential for meiotic chromosome condensation and separation in mice
Li X M, et al.
Biology of Reproduction, 89(5), 1273-1282 (2013)
N Hajji et al.
Mutation research, 530(1-2), 35-46 (2003-10-18)
The bis-dioxopiperazine ICRF-193 has long time been considered as a pure topoisomerase II catalytic inhibitor able to exert its inhibitory effect on the enzyme without stabilization of the so-called cleavable complex formed by DNA covalently bound to topoisomerase II. In
ICRF-193, a catalytic inhibitor of DNA topoisomerase II, delays the cell cycle progression from metaphase, but not from anaphase to the G1 phase in mammalian cells
Iwai M, et al.
Febs Letters, 406(3), 267-270 (1997)
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