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Synonyms | AK-01 | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C24H26ClF2N5O2 |
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分子量 | 489.95 | CAS No. | 1919888-06-4 | |
Solubility (25°C)* | 体外 | DMSO | 98 mg/mL (200.02 mM) | |
Ethanol | 15 mg/mL (30.61 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | LY3295668 (AK-01) is a potent, orally active and specific inhibitor of Aurora A kinase with Ki of 0.8 nM and 1038 nM for AURKA and AURKB, respectively. |
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in vitro | LY3295668, an AURKA inhibitor with over 1,000-fold selectivity versus AURKB, is distinguished by minimal toxicity to bone marrow cells at concentrations active against RB1mut cancer cells.[1] |
in vivo | LY3295668 leads to durable regression of RB1mut tumor xenografts at exposures that are well tolerated in rodents. Genetic suppression screens identifi ed enforcers of the spindle-assembly checkpoint (SAC) as essential for LY3295668 cytotoxicity in RB1-defi cient cancers and suggest a model in which a primed SAC creates a unique dependency on AURKA for mitotic exit and survival.[1] |
細胞アッセイ | 細胞株 | NCI-H446 cells, Calu-6 cells |
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濃度 | 0.001 μM - 1 μM | |
反応時間 | 24 h, 48 h, 72 h | |
実験の流れ | To measure apoptosis by IncuCyte Zoom instrument, NCI-H446 and Calu-6 cells are plated on Costar 3596 plates and treated with LY3295668 at different concentrations for 24, 48, and 72 hours. Caspase 3/7 activation is measured with Cell- Player 96-Well Kinetic Caspase 3/7 reagent. Green fluorescent images are acquired every 2 hours. Green objects counted (y-axis) are plotted against either real time (x-axis) or raw numbers as percent control. |
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動物実験 | 動物モデル | 7–8 week-old athymic nude female mice |
投薬量 | 50 mg/kg | |
投与方法 | Oral gavage |
Combination drug screen targeting glioblastoma core vulnerabilities reveals pharmacological synergisms [ EBioMedicine, 2023, 95:104752] | PubMed: 37572644 |
BCL-xL inhibition potentiates cancer therapies by redirecting the outcome of p53 activation from senescence to apoptosis [ Cell Rep, 2022, 41(12):111826] | PubMed: 36543138 |
Treatment of RB-deficient retinoblastoma with Aurora-A kinase inhibitor [ Kaohsiung J Med Sci, 2021, 10.1002/kjm2.12469] | PubMed: 34741392 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。