Aurora A-IN-5
Aurora A-IN-5 is a potent and highly selective Aurora A inhibitor (IC50 = 0.02 μM), showing 362-fold selectivity for over Aurora B. Aurora A-IN-5 shows its selectivity through unique C−H/π interactions, enhanced hydrophobic contacts, an open binding pocket, and tighter protein packing. Aurora A-IN-5 suppresses Aurora A autophosphorylation, thereby inhibiting cancer cell proliferation by inducing G2/M phase arrest, triggering apoptosis, and suppressing colony formation. Aurora A-IN-5 inhibits tumor growth in MDA-MB-231 xenograft mouse models. Aurora A-IN-5 can be used for breast, cervical, prostate, and lymphoma cancer research.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C25H29N7O2
- 分子量:459.54
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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 0.02 μM (IC50) |
体外実験
Aurora A-IN-5 (compound 5h) (48 h) shows strong antiproliferative activity against a panel of cancer cell lines, with IC50 values of 2.87 μM (K562), 1.50 μM (MCF-7), 0.85 μM (HeLa), 1.85 μM (DU145), 2.25 μM (MOLT-4), and 2.04μM (MDA-MB-231)[1].
Aurora A-IN-5 (0.5 μM, 48 h) causes abnormalities in spindle morphology and chromosomal organization in MDA-MB-231 cells[1].
Aurora A-IN-5 (2.5-10 μM, 24 h) effectively inhibits MDA-MB-231 cell division by halting cell cycle progression at the G2/M phase[1].
Aurora A-IN-5 (2-20 μM, 24 h) induces apoptosis in MDA-MB-231 cells in a dose-dependent manner[1].
Aurora A-IN-5 (2 μM, 14 days) effectively suppresses colony formation in MDA-MB-231 cells, thus inhibiting their proliferation[1].
Aurora A-IN-5 (0-1 μM) exhibits potent, selective, and dose-dependent inhibition of Aurora A phosphorylation at Thr288, with concurrent demonstration of target engagement in MDA-MB-231 cells through significant stabilization of Aurora A protein in a cellular thermal shift assay (46-62 °C)[1].
Aurora A-IN-5 exhibits toxicity in mouse embryonic osteoblast MC3T3-E1 cells (IC50 = 7.135 μM) but exhibits minimal toxicity toward normal liver LO2 cells (IC50 = 43.86 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:2.0 μM
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Incubation Time:14 days
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Result:Showed considerably fewer colonies (26 ± 3) compared to the untreated control group (106 ± 3).
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Cell Line:MDA-MB-231 cells
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Concentration:2.0 and 20.0 μM
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Incubation Time:24 h
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Result:Displayed a concentration-dependent increase in apoptotic cells, ranging from 11.5% at 2.0 μM to 88.6% at 20.0 μM.
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Cell Line:MDA-MB-231 cells
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Concentration:2.5, 5.0 and 10.0 μM
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Incubation Time:24 h
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Result:Showed a significant ability to arrest MDA-MB-231 cells in the G2/M phase.
The percentage of cells in the G2/M phase gradually increased from 24.2% to 61.8% at 2.5 μM.
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Cell Line:MDA-MB-231 cells
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Concentration:0.5 μM
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Incubation Time:48 h
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Result:Displayed abnormal spindle configurations, either monopolar or multipolar, accompanied by various aberrations in chromosome alignment.
Parmacokinetics
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:Female BALB/c nude mice (1-5 weeks) subcutaneously injected with MDA-MB-231 cells[1]
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Dosage:30 mg/kg
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Administration:i.p., every two days for 20 days
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Result:Achieved a tumor growth inhibition rate of 73.0%.
Exhibited slightly increased body weight without any significant fluctuations throughout the treatment duration.
Revealed no significant parenchymal damage or inflammatory cell infiltration in vital organs such as the heart, liver, spleen, lung, and kidney.
- Somatic Cell Culture
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Apoptosis Solutions
- Soft Agar Colony Formation Assay
- MTT Cell Proliferation Assay
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Patient-Derived Xenograft (PDX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
化学情報
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分子量 459.54
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分子式 C25H29N7O2
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SMILES
CN1CCN(C2=CC3=NC(C4=CC=CC(OC)=C4OC)=NC(NC5=NNC(C)=C5)=C3C=C2)CC1
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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)
Aurora A-IN-5 関連分類
HY-178343 関連分類
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