I4659
ICRF-193
synthetic (organic), ≥95%, topoisomerase II inhibitor, solid,powder or flakes
别名:
meso-4,4′-(3,2-丁二基)-双(2,6-哌嗪二酮)
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关于此项目
经验公式（希尔记法）:
C12H18N4O4
化学文摘社编号:
分子量:
282.30
MDL编号:
UNSPSC代码:
12352204
PubChem化学物质编号:
NACRES:
NA.77
产品名称
ICRF-193, apoptosis inducer, arabinosidase substrate
生物来源
synthetic (organic)
质量水平
方案
≥95%
表单
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
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
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
B B Hasinoff et al.
Molecular pharmacology, 59(3), 453-461 (2001-02-17)
The bisdioxopiperazines ICRF-187 (dexrazoxane), ICRF-193, and ICRF-154 are catalytic noncleavable complex-forming inhibitors of DNA topoisomerase II that do not produce protein-linked DNA strand breaks. In this study, we showed that bisdioxopiperazines induced erythroid differentiation, inhibited human leukemia K562 cell growth
Sílvia Dyson et al.
The EMBO journal, 40(1), e105393-e105393 (2020-11-07)
The juxtaposition of intracellular DNA segments, together with the DNA-passage activity of topoisomerase II, leads to the formation of DNA knots and interlinks, which jeopardize chromatin structure and gene expression. Recent studies in budding yeast have shown that some mechanism
K C Huang et al.
The Journal of biological chemistry, 276(48), 44488-44494 (2001-09-29)
Antineoplastic bis(dioxopiperazine)s, such as meso-2,3-bis(2,6-dioxopiperazin-4-yl)butane (ICRF-193), are widely believed to be only catalytic inhibitors of topoisomerase II. However, topoisomerase inhibitors have little or no antineoplastic activity unless they are topoisomerase poisons, a special subclass of topoisomerase-targeting drugs that stabilize topoisomerase-DNA
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)
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
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