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 番号: 1192754-38-3
- 分子式: C34H36N6O4
- 分子量:592.70
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Aurora Kinase アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
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 |
|---|---|---|---|---|
| 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] |
体外実験
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.
体内実験
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.
化学情報
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CAS 番号 1192754-38-3
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分子量 592.70
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
IBPR002 関連分類
HY-165369 関連分類
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