Centrinone (LCR-263)

製品コードS7837 バッチS783702

印刷

化学情報

Synonyms

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₆H₂₅F₂N₇O₆S₂

分子量

633.65

CAS No.

1798871-30-3

Solubility (25°C)*

体外

DMSO

100 mg/mL (157.81 mM)

Water

Insoluble

Ethanol

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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.650mg/ml (2.60mM)	Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.830mg/ml (1.31mM)	Taking the 1 mL working solution as an example, add 50 μL of 16.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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	Centrinone (LCR-263) is a selective and reversible polo-like kinase 4 (PLK4) inhibitor with Ki of 0.16 nM.
in vitro	Centrinone (LCR-263) prevents centriole assembly by inhibiting Plk4Centrinone treatment causes centrosome depletion in human and other vertebrate cells.<sup><a class="sref" href="#s_ref">[1]</a></sup>

プロトコル(参考用のみ)

キナーゼアッセイ
キナーゼアッセイ	Purified 6xHis-tagged human Plk4 kinase domain is in 20 mM Tris pH 7.5, 100 mM NaCl, 10% glycerol, 1 mM DTT. 2X reaction buffer consists of 50 mM HEPES pH 8.5, 20 mM MgCl2, 1 mM DTT, 0.2 mg/mL BSA, 16 μM ATP, and 200 μM A-A11 substrate. The Plk4 concentration in the final reaction is 2.5-10 nM with a final pH of 8.0. Centrinone array in dose response are added from DMSO stocks. Reactions are allowed to proceed for 4-16 hours at 25°C. Detection is performed using ADP-Glo reagent. Luminescence is measured on an plate reader.
細胞アッセイ	細胞株	HeLa cells, NIH/3T3 cells
	濃度	125 nM
	反応時間	2 weeks
	実験の流れ	For the first two days after centrinone addition, when cells retained 2 or 1 centrosomes, the proliferation of HeLa and NIH/3T3 cells was identical to controls; this was followed by a decrease in proliferation rate coincident with the appearance of centrosome-less cells. Long-term treated cells continued to proliferate at the slower rate, and returned to the control rate after wash-out-mediated centrosome recovery.

参考

https://pubmed.ncbi.nlm.nih.gov/25931445/

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：

Unraveling the impact of crizotinib to promote megakaryopoiesis for alleviating thrombocytopenia in myelodysplastic neoplasms [ Leukemia, 2025, 10.1038/s41375-025-02729-w]	PubMed: 40813622
Pericentriolar material 1 aggregation maintains cell survival upon prolonged replication stress [ Arch Biochem Biophys, 2025, 768:110383]	PubMed: 40090437

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。