1. Cell Cycle/DNA Damage Epigenetics
  2. Aurora Kinase
  3. IBPR002

IBPR002 是一种 Aurora kinase AAurora kinase B 抑制剂,其 IC50 分别为 41 nM 和 17 nM。IBPR002 可破坏动粒微管的成核与成束,破坏有丝分裂纺锤体的双极性,并促使非磷酸化人肝癌上调蛋白 (HURP) 与母中心体来源的微管结合。IBPR002 可降低无胸腺裸鼠结直肠癌异种移植模型中的肿瘤发生水平。IBPR002 可用于结直肠癌的相关研究。

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IBPR002

IBPR002 Chemical Structure

CAS No. : 1192754-38-3

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生物活性

IBPR002 is an inhibitor of Aurora kinase A and Aurora kinase B, with IC50 values of 41 nM and 17 nM, respectively. IBPR002 disrupts the nucleation and bundling of kinetochore microtubules, impairs the bipolarity of mitotic spindles, and promotes the binding of non-phosphorylated hepatoma up-regulated protein (HURP) to microtubules derived from the mother centrosome. IBPR002 reduces tumorigenesis levels in a colorectal cancer xenograft model using athymic nude mice. IBPR002 is applicable for research related to colorectal cancer[1].

IC50 & Target[1]

Aurora A

41 nM (IC50)

Aurora B

17 nM (IC50)

体外研究
(In Vitro)

IBPR002 (1.0 μM; 13 h) 会破坏双极纺锤体的形成,并将未磷酸化的 HURP 限制在中心体微管的负极,从而在 HeLa 细胞中诱导出三种不同的有丝分裂表型[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Immunofluorescence[1]

Cell Line: HeLa cells
Concentration: 1.0 μM
Incubation Time: 13 h (after thymidine release)
Result: Induced three distinct HURP localization phenotypes: ~20% of cells showed a monoastral spindle with HURP surrounding unseparated centrosomes (Phenotype-1), the majority showed HURP associated with centrosomal microtubules projecting toward chromosomes from one separated centrosome (Phenotype-2) or both separated centrosomes (Phenotype-3).
Disrupted bipolar spindle formation.
Restricted HURP to the minus ends of centrosomal microtubules, unlike control cells where HURP localizes to both ends of microtubules.
体内研究
(In Vivo)

IBPR002 (50 mg/kg;静脉注射;每周给药 5 次,连续 2 周) 可显著抑制雄性无胸腺裸鼠体内 HCT116 结直肠癌移植瘤的生长[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: athymic nude (male)[1]
Dosage: 50 mg/kg
Administration: i.v.; five daily doses per week; two consecutive weeks
Result: Significantly inhibited growth of xenograft colorectal cancer cells, with mean tumor volume at study end being substantially lower than vehicle control levels.
分子量

592.70

Formula

C34H36N6O4

CAS 号
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.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
IBPR002
目录号:
HY-165369
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