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 Chemische Struktur

CAS. Nr. : 1192754-38-3

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Beschreibung

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)

Cellular Effect
Cell Line Type Value Description References
HCT-116 EC50
195 nM
Compound: 35, IBPR002
Antiproliferative activity against human HCT116 cells
Antiproliferative activity against human HCT116 cells
[PMID: 23808327]
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.
Molekulargewicht

592.70

Formel

C34H36N6O4

CAS. Nr.
SMILES

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

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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