AI-10-49

製品コードS7814 バッチS781402

印刷

化学情報

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

C30H22F6N6O5
分子量 660.52 CAS No. 1256094-72-0
Solubility (25°C)* 体外 DMSO 100 mg/mL (151.39 mM)
Ethanol (warmed with 50ºC water bath) 100 mg/mL (151.39 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
10%DMSO 40%PEG300 5%Tween80 45%ddH2O
2.5mg/ml Taking the 1 mL working solution as an example, add 100 μL of 25 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 450 μL of ddH2O to adjust the volume to 1 mL. 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 AI-10-49 is a selective inhibitor of the binding of CBFβ-SMMHC to RUNX1 with IC50 of 260 nM.
in vitro AI-10-49 displays specific growth inhibition of inv(16)-positive cell line ME-1. AI-10-49 selectively binds to CBFβ-SMMHC, disrupts its binding to RUNX1, and restores RUNX1 transcriptional activity. [1]
in vivo In mice transplanted with Cbfb+/MYH11;Nras+/G12D leukemic cells, AI-10-49 (200 mg/kg, i.p.) reduces leukemia expansion. [1]

プロトコル(参考用のみ)

キナーゼアッセイ FRET assays
Cerulean-Runt domain is expressed and purified. Venus-CBFβ-SMMHC is constructed by inserting 6xHis tag and Venus into pET22b vector between NdeI and NcoI sites, and by inserting CBFβ-SMMHC (the CBFβ-SMMHC construct contains 369 amino acids, 1-166 from CBFβ and 166-369 from MYH11 (amino acids 1526-1730)) between the NcoI and BamHI sites. The fusion protein is purified by standard Ni-affinity chromatography with an on column benzonase treatment to remove residual DNA contaminants. Proteins are dialyzed into FRET buffer (25mM Tris-HCl, pH 7.5, 150mM KCl, 2mM MgCl2) prior to use. Protein concentrations are determined by UV absorbance of the Cerulean and Venus at 433 and 513 nm, respectively. Cerulean-Runt domain and Venus-CBFβ-SMMHC were mixed 1:1 to achieve a final concentration of 10 nM in 96 well black COSTAR plates. DMSO solutions of compounds are added to a final DMSO concentration of 5% (v/v) and the plates incubated at room temperature for one hour in the dark. A PHERAstar microplate reader is used to measure fluorescence (excitation at 433 nm and emission measured at 474 and 525 nm). For IC50 determinations, the ratios of the fluorescence intensities at 525 nm and 474 nm are plotted versus the log of compound concentration, and the resulting curve was fit to a sigmoidal curve using Origin7.0. Three independent measurements are performed and their average and deviation are used for IC50 data fitting.
細胞アッセイ 細胞株 HL-60, KG-1, THP-1, Kasumi-1, TUR 9, U937, and MOLM-13 cells
濃度 ~10 μM
反応時間 48 hours
実験の流れ Cell lines are cultured in IMDM supplemented with 10%~20% fetal bovine serum (FBS) according to culture conditions indicated by ATCC and 1% penicillin/streptomycin (Pen/Strep). All cell lines are tested for mycoplasma. Cells are cultured at 300,000 cells per ml in 96 well plates for 24 and 48 hours in DMSO, or different of AI-10-47, AI-410-49, AI-4-57, or AI-4-88); each in duplicate or triplicate. Cell viability is evaluated using DAPI by flow cytometry. Data is analyzed using FlowJo software and Graphpad Prism software.
動物実験 動物モデル Mice transplanted with Cbfb+/MYH11;Nras+/G12D leukemic cells
投薬量 200 mg/kg
投与方法 i.p.

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。