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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- CAS No.: 1192754-38-3
- Formule: C34H36N6O4
- Masse moléculaire:592.70
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Stockage:
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
[1]|
Aurora A 41 nM (IC50) |
Aurora B 17 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HCT-116 | EC50 |
195 nM
Compound: 35, IBPR002
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Antiproliferative activity against human HCT116 cells
Antiproliferative activity against human HCT116 cells
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[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.
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Cell Line:HeLa cells
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Concentration:1.0 μM
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Incubation Time:13 h (after thymidine release)
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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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:athymic nude (male)[1]
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Dosage:50 mg/kg
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Administration:i.v.; five daily doses per week; two consecutive weeks
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Result:Significantly inhibited growth of xenograft colorectal cancer cells, with mean tumor volume at study end being substantially lower than vehicle control levels.
Chemical Information
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CAS No. 1192754-38-3
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Masse moléculaire 592.70
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Formule C34H36N6O4
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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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
IBPR002 Related Classifications
HY-165369 Related Classifications
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