Ro3280

製品コードS7248 バッチS724801

印刷

化学情報

Chemical Structure Synonyms Ro5203280 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C27H35F2N7O3
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
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 RO3280 (Ro5203280) is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM.
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.

プロトコル(参考用のみ)

動物実験 動物モデル Human colorectal cancer xenografts HT-29
投薬量 40 mg/kg
投与方法 q4d i.v.

参考

  • https://pubmed.ncbi.nlm.nih.gov/22172702/

カスタマーフィードバック

Data from [Data independently produced by , , J Cell Mol Med, 2017, 21(4):758-767]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

CETP inhibition enhances monocyte activation and bacterial clearance and reduces streptococcus pneumonia-associated mortality in mice [ JCI Insight, 2024, 9(8)e173205] PubMed: 38646937
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。