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

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.

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IBPR002

IBPR002 Chemical Structure

CAS No. : 1192754-38-3

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Description

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)

In Vitro

IBPR002 (1.0 μM; 13 h) disrupts bipolar spindle formation and restricts unphosphorylated HURP to the minus ends of centrosomal microtubules, inducing three distinct mitotic phenotypes in HeLa cells[1].

MedChemExpress (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.
In Vivo

IBPR002 (50 mg/kg; i.v.; five daily doses per week; two consecutive weeks) significantly inhibits growth of HCT116 colorectal cancer xenografts in male athymic nude mice[1].

MedChemExpress (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.
Molecular Weight

592.70

Formula

C34H36N6O4

CAS No.
SMILES

O=C(NC=1C=CC=CC1)NC2=CC=C(C=C2)CCNC=3N=CN=C4OC(=CC43)C=5C=CC(OCCN6CCC(O)CC6)=CC5

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    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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IBPR002
Cat. No.:
HY-165369
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