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Synonyms | Ro5203280 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C27H35F2N7O3 |
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分子量 | 543.61 | CAS No. | 1062243-51-9 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (183.95 mM) | |
Ethanol | 100 mg/mL (183.95 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 | RO3280 (Ro5203280) is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM. |
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in vitro | RO3280 shows the strong anti-proliferative activity against lung cancer cell line H82, colorectal cancer cell HT-29, breast cancer cell MDA-MB-468, prostate cancer cell PC3 and skin cancer cell A375 with IC50s of 5, 10, 19, 12 and 70 nM, respectively. [1] |
in vivo | RO3280 displays robust antitumor activity in nude mouse implanted with HT-29 human colorectal tumors ranging from 72% tumor growth inhibition when dosed once weekly at 40 mg/kg, to complete tumor regression when dosed more frequently.. [1] |
特徴 | A selective PLK1 inhibitor. Demonstrates greater potency than BI2536. Potential use in nasopharyngeal carcinomas. |
動物実験 | 動物モデル | Human colorectal cancer xenografts HT-29 |
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投薬量 | 40 mg/kg | |
投与方法 | q4d i.v. |
Data from [Data independently produced by , , J Cell Mol Med, 2017, 21(4):758-767]
Inhibition of PLK1 Destabilizes EGFR and Sensitizes EGFR-Mutated Lung Cancer Cells to Small Molecule Inhibitor Osimertinib [ Cancers (Basel), 2023, 15(9)2589] | PubMed: 37174055 |
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors [ J Med Chem, 2021, 10.1021/acs.jmedchem.1c01096] | PubMed: 34710325 |
Targeting Polo-like kinase 1 and TRAIL enhances apoptosis in non-small cell lung cancer [ Oncotarget, 2018, 9(47):28731-28744] | PubMed: 29983892 |
Targeted inhibition of Polo-like kinase 1 by a novel small-molecule inhibitor induces mitotic catastrophe and apoptosis in human bladder cancer cells. [Zhang Z, et al. J Cell Mol Med, 2017, 21(4):758-767] | PubMed: 27878946 |
Molecular targeting of the oncoprotein PLK1 in pediatric acute myeloid leukemia: RO3280, a novel PLK1 inhibitor, induces apoptosis in leukemia cells. [ Int J Mol Sci, 2015, 16(1):1266-92] | PubMed: 25574601 |
Mitotic entry: Non-genetic heterogeneity exposes the requirement for Plk1 [Aspinall CF, et al. Oncotarget, 2015, 6(34):36472-88] | PubMed: 26472023 |
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。