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87099-50-1

中文名称 Isofistularin-3
CAS 87099-50-1
分子式 C31H30Br6N4O11
分子量 1114.01
MOL 文件 87099-50-1.mol
87099-50-1 结构式 87099-50-1 结构式

基本信息

英文别名
Isofistularin-3
1-Oxa-2-azaspiro[4.5]deca-2,6,8-triene-3-carboxamide, 7,9-dibromo-N-[(2R)-3-[2,6-dibromo-4-[2-[[[(5S,10R)-7,9-dibromo-10-hydroxy-8-methoxy-1-oxa-2-azaspiro[4.5]deca-2,6,8-trien-3-yl]carbonyl]amino]-1-hydroxyethyl]phenoxy]-2-hydroxypropyl]-10-hydroxy-8-methoxy-, (5S,10R)-

物理化学性质

密度2.19±0.1 g/cm3(Predicted)
酸度系数(pKa)10.66±0.70(Predicted)
形态白色至类白色无定形固体

安全数据

危险性符号(GHS)GHS hazard pictograms
GHS07
警示词警告
危险性描述H315-H319-H335
防范说明P271-P261

常见问题列表

生物活性
Isofistularin-3 ((+)-11-epi-Fistularin 3) 是一种直接的 DNA 竞争性 DNMT1 抑制剂,IC50 为 13.5 μM。Isofistularin-3 作为 DNA 去甲基化剂,可诱导肿瘤细胞周期阻滞和 TRAIL 致敏。Isofistularin-3 可作用做抗体偶联药物 (ADC) 的毒素部分。
靶点

DNMT1

13.5 μM (IC 50 )

Traditional Cytotoxic Agents

体外研究

Isofistularin-3 (1-50 μM; 24-72 hours) shows a marked reduction of cell proliferation.
Isofistularin-3 (5-50 μM; 24 hours) increases arrests cancer cells in G0/G1 cell cycle phase.
Isofistularin-3 (25 μM; 72 hours) increases AHR expression. Isofistularin-3 induces AHR promoter demethylation. Isofistularin-3 (72 hours) inhibits a broader panel of cancer cell lines proliferation, with the GI 50 s ranging from 7.3-14.8 μM. Isofistularin-3 induces morphological changes and autophagy in RAJI cells. Isofistularin-3 induces caspase-dependent and -independent cell death. Isofistularin-3 sensitizes lymphoma cells to TRAIL-induced apoptosis.

Cell Proliferation Assay

Cell Line: RAJI and U-937 lymphoma cells
Concentration: 1, 5, 15, 25, 50 μM
Incubation Time: 24 and 72 hours
Result: A marked reduction of cell proliferation.

Cell Cycle Analysis

Cell Line: RAJI and U-937 cells
Concentration: 5, 50 μM
Incubation Time: 24 hours
Result: An arrest in the G0/G1 phase of the cell cycle for both cell lines.

RT-PCR

Cell Line: RAJI cells
Concentration: 25 μM
Incubation Time: 72 h
Result: AHR mRNA expression level was 5.1 times higher.
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