K03861 (AUZ454)

製品コードS8100 バッチS810002

印刷

化学情報

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

C24H26F3N7O2
分子量 501.50 CAS No. 853299-07-7
Solubility (25°C)* 体外 DMSO 100 mg/mL (199.4 mM)
Ethanol 15 mg/mL (29.91 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 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 95% Corn oil
1.25mg/ml Taking the 1 mL working solution as an example, add 50 μL of 25 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 K03861 (AUZ454) is a type II CDK2 inhibitor with Kd of 50 nM, 18.6 nM, 15.4 nM, and 9.7 nM for CDK2(WT), CDK2(C118L), CDK2(A144C), and CDK2(C118L/A144C), respectlvely.
in vitro K03861 inhibits CDK2 activity by competing with binding of activating cyclins. [1]

プロトコル(参考用のみ)

キナーゼアッセイ Enzymatic Assays
A microfluidic electrophoretic mobility-shift assay is used to determine activities of the kinases, observe the effects of mutations and establish kinetic parameters of binding. The assay is based on the electrophoretic separation of phosphorylated (product) and nonphosphorylated (substrate) peptides based on their charge difference. The peptides are tagged with fluorescent marker and the shift in mobility is detected via laser-induced fluorescence allowing for direct and real-time measurements of kinase activities (sequence for CDK2:5-FAM-QSPKKG-CONH2). Results are expressed as a conversion ratio by measuring peak heights for both the substrate and product and dividing the product peak height by the sum of peak heights for both substrate and product. Concentrations for the enzyme and ATP are assay specific and optimized for each kinase individually during assay optimization. The assay optimization started with determination of the lowest protein concentration that provides sufficient signal for analysis under conditions of saturating peptide and ATP. This is done to ensure a steady linear reaction with substrate consumption less than 20% so that the initial enzymatic velocity (V) follows the Michaelis–Menten equation. Next, the apparent Michaelis constants for ATP (Km ATP) and peptide (Km peptide) are obtained from measurements conducted at constant enzyme concentration and a range of ATP and peptide concentrations respectively, and the kcat values are calculated.

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：

Functional Differentiation of Cyclins and Cyclin-Dependent Kinases in Giardia lamblia [ Microbiol Spectr, 2023, 11(2):e0491922] PubMed: 36877015
Genetic instability from a single S phase after whole-genome duplication [ Nature, 2022, 604(7904):146-151] PubMed: 35355016
p53 directs leader cell behavior, migration, and clearance during epithelial repair [ Science, 2022, 375(6581):eabl8876] PubMed: 35143293
Icaritin inhibits CDK2 expression and activity to interfere with tumor progression [ iScience, 2022, 25(9):104991] PubMed: 36093042
Comprehensive drug response profiling and pan-omic analysis identified therapeutic candidates and prognostic biomarkers for Asian cholangiocarcinoma [ iScience, 2022, 25(10):105182] PubMed: 36248745
Transient inhibition of CDK2 activity prevents oocyte meiosis I completion and egg activation in mouse [ J Cell Physiol, 2022, 10.1002/jcp.30885] PubMed: 36161883
Postnatal expression and possible function of RANK and RANKL in the murine inner ear [ Bone, 2021, 145:115837] PubMed: 33385614
Tumors driven by RAS signaling harbor a natural vulnerability to oncolytic virus M1 [ Mol Oncol, 2020, 14(12):3153-3168] PubMed: 33037696
Tumors driven by RAS signaling harbor a natural vulnerability to oncolytic virus M1 [ Mol Oncol, 2020, 14(12):3153-3168] PubMed: 33037696
Bromodomain-Containing Protein BRD4 Is Hyperphosphorylated in Mitosis [ Cancers (Basel), 2020, 12(6):E1637] PubMed: 32575711

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。