SP-96

SP-96 is a potent, selective and non-ATP-competitive inhibitor of Aurora B with IC50 of 0.316 nM. SP-96 can be used for the research of triple negative breast cancer (TNBC).

SP-96化学構造

CAS No. 2682114-54-9

サイズ 価格(税別) 在庫状況
JPY 32500 国内在庫あり
JPY 98500 国内在庫あり

代表番号: 045-509-1970|電子メール:[email protected]
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文献中Selleckの製品使用例(1)

製品安全説明書

現在のバッチを見る: S965801 DMSO] 91 mg/mL] false] Ethanol] 2 mg/mL] false] Water] Insoluble] false 純度: 99.77%
99.77

SP-96関連製品

Aurora Kinase阻害剤の選択性比較

生物活性

製品説明 SP-96 is a potent, selective and non-ATP-competitive inhibitor of Aurora B with IC50 of 0.316 nM. SP-96 can be used for the research of triple negative breast cancer (TNBC).
Targets
Aurora B [1]
(Cell-free assay)
0.316 nM
In Vitro
In vitro

SP-96 shows sub-nanomolar potency in Aurora B enzymatic assays (IC50 = 0.316 ± 0.031 nM). SP-96 shows >2000 fold selectivity against FLT3 and KIT which is important for normal hematopoiesis. Enzyme kinetics of SP-96 shows non-ATP competitive inhibition which makes it a first-in-class inhibitor. SP-96 shows selective growth inhibition in NCI60 screening, including inhibition of MDA-MD-468, a Triple Negative Breast Cancer cell line.[1]

Kinase Assay Aurora Kinase B enzymatic assay
Kinase inhibition assay is done by measuring kinase activity in a microfluidics assay. The separation of a phosphorylated product from substrate is monitored. The assay is run using a 12-sipper chip on a Caliper EZ Reader II. The recipe used for separation buffer is 100 mM HEPES, 10 mM EDTA, 0.015% Brij-35, 0.1% CR-3. The compound stocks (20 mM in DMSO) are diluted into kinase buffer. 1 μL of desired stock solution is transferred into a 384-well microtiter assay plate. The Aurora B enzyme is diluted in kinase buffer to a concentration of 2 nM. 5 μL of the enzyme mixture is transferred to the assay plate. The inhibitors/Aurora B enzyme are incubated for 60 min with minor shaking. A substrate mix is prepared containing ATP and 5FAM tagged peptide dissolved in kinase buffer described above. 5 μL of the substrate solution is added to the assay plate. Running concentrations are as follows: peptide (1.5 μM), ATP (190 μM), and compound 12-point ½log dilutions (0.2 mM-0.632 nM). No inhibitor is added for positive control, and no enzymewas added for negative control. For running control, barasertib is used. Percentage inhibition is measured by comparing starting peptide to phosphorylated productpeaks.
細胞実験 細胞株 MCF-7 cells
濃度 --
反応時間 24 h
実験の流れ

The growth inhibition of 60 cell lines is obtained by submitting the compound to National Cancer Institute’s NCI60 panel. MCF-7 cells are cultured in RPMI-1640 medium with 5% FBS in an incubator maintained at 37 ℃ and 5% CO2. The media is changed on alternate days. After reaching confluency, the media is aspirated, cells are washed with PBS, detached using 0.25% trypsin and centrifuged. The collected cells are seeded in 96-well microtiter plates at a density of 5000 cells/well. The cells are allowed to adhere to plate overnight. The test compounds, vehicle control and positive controls are added 24 h after the cells are plated and allowed to incubate. Following 24 h of incubation, the media is aspirated, and the cells are washed with PBS. 40 mL of the media and 10 mL of 5 mg/mL of MTT solution prepared in PBS is added to the cells and incubated for 4 h at 37 ℃ and 5% CO2. After incubation, 150 mL of DMSO is added to each well and the cell viability is measured at 570 nM by an ELISA plate reader.

化学情報

分子量 453.47 化学式

C25H20FN7O

CAS No. 2682114-54-9 SDF --
Smiles CC1N=CC(=N1)C2=CC=C3C(=NC=NC3=C2)NC4=CC=CC(=C4)NC(=O)NC5=CC(=CC=C5)F
保管 3 years -20°C powder

In vitro
Batch:

DMSO : 91 mg/mL ( (200.67 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 2 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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