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AZD6482
別名：KIN-193
AZD6482 (KIN-193) is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ in cell-free assays. Phase 1.
CAS No. 1173900-33-8
文献中Selleckの製品使用例（24）
カスタマーフィードバック4个实验数据
製品安全説明書
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純度：
99.92%
99.92
AZD6482関連製品
シグナル伝達経路
PI3K阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| human MAD-MB-468 cells | Function assay | Inhibition of PI3Kbeta in human MAD-MB-468 cells assessed as inhibition of Ser473 Akt phosphorylation by cellular potency assay, IC50=0.04 μM | 24992874 | ||
| human MDA-MB-361 cell | Growth inhibition assay | Inhibition of human MDA-MB-361 cell growth in a cell viability assay, IC50=3.52709 μM | SANGER | ||
| human NCI-H1755 cell | Growth inhibition assay | Inhibition of human NCI-H1755 cell growth in a cell viability assay, IC50=3.27063 μM | SANGER | ||
| human NCI-H2030 cell | Growth inhibition assay | Inhibition of human NCI-H2030 cell growth in a cell viability assay, IC50=2.90288 μM | SANGER | ||
| human SF295 cell | Growth inhibition assay | Inhibition of human SF295 cell growth in a cell viability assay, IC50=2.76955 μM | SANGER | ||
| human SW1088 cell | Growth inhibition assay | Inhibition of human SW1088 cell growth in a cell viability assay, IC50=2.48143 μM | SANGER | ||
| human GDM-1 cell | Growth inhibition assay | Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=2.24206 μM | SANGER | ||
| human COLO-684 cell | Growth inhibition assay | Inhibition of human COLO-684 cell growth in a cell viability assay, IC50=2.20032 μM | SANGER | ||
| human D-542MG cell | Growth inhibition assay | Inhibition of human D-542MG cell growth in a cell viability assay, IC50=1.85077 μM | SANGER | ||
| human HSC-2 cell | Growth inhibition assay | Inhibition of human HSC-2 cell growth in a cell viability assay, IC50=1.75727 μM | SANGER | ||
| human EB2 cell | Growth inhibition assay | Inhibition of human EB2 cell growth in a cell viability assay, IC50=1.75019 μM | SANGER | ||
| human LoVo cell | Growth inhibition assay | Inhibition of human LoVo cell growth in a cell viability assay, IC50=1.73825 μM | SANGER | ||
| human D-336MG cell | Growth inhibition assay | Inhibition of human D-336MG cell growth in a cell viability assay, IC50=1.6688 μM | SANGER | ||
| human SNB75 cell | Growth inhibition assay | Inhibition of human SNB75 cell growth in a cell viability assay, IC50=1.66508 μM | SANGER | ||
| human HCC70 cell | Growth inhibition assay | Inhibition of human HCC70 cell growth in a cell viability assay, IC50=1.66146 μM | SANGER | ||
| human 639-V cell | Growth inhibition assay | Inhibition of human 639-V cell growth in a cell viability assay, IC50=1.63144 μM | SANGER | ||
| human HuO9 cell | Growth inhibition assay | Inhibition of human HuO9 cell growth in a cell viability assay, IC50=1.6128 μM | SANGER | ||
| human KU812 cell | Growth inhibition assay | Inhibition of human KU812 cell growth in a cell viability assay, IC50=1.59628 μM | SANGER | ||
| human OCUB-M cell | Growth inhibition assay | Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=1.58314 μM | SANGER | ||
| human NCI-H2291 cell | Growth inhibition assay | Inhibition of human NCI-H2291 cell growth in a cell viability assay, IC50=1.5761 μM | SANGER | ||
| human SNU-423 cell | Growth inhibition assay | Inhibition of human SNU-423 cell growth in a cell viability assay, IC50=1.57192 μM | SANGER | ||
| human MFE-296 cell | Growth inhibition assay | Inhibition of human MFE-296 cell growth in a cell viability assay, IC50=1.56836 μM | SANGER | ||
| human LXF-289 cell | Growth inhibition assay | Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=1.55104 μM | SANGER | ||
| human NB12 cell | Growth inhibition assay | Inhibition of human NB12 cell growth in a cell viability assay, IC50=1.54842 μM | SANGER | ||
| human MDA-MB-468 cell | Growth inhibition assay | Inhibition of human MDA-MB-468 cell growth in a cell viability assay, IC50=1.53736 μM | SANGER | ||
| human MC116 cell | Growth inhibition assay | Inhibition of human MC116 cell growth in a cell viability assay, IC50=1.46122 μM | SANGER | ||
| human CCF-STTG1 cell | Growth inhibition assay | Inhibition of human CCF-STTG1 cell growth in a cell viability assay, IC50=1.42525 μM | SANGER | ||
| human Becker cell | Growth inhibition assay | Inhibition of human Becker cell growth in a cell viability assay, IC50=1.36315 μM | SANGER | ||
| human GI-1 cell | Growth inhibition assay | Inhibition of human GI-1 cell growth in a cell viability assay, IC50=1.31808 μM | SANGER | ||
| human 786-0 cell | Growth inhibition assay | Inhibition of human 786-0 cell growth in a cell viability assay, IC50=1.31283 μM | SANGER | ||
| human HAL-01 cell | Growth inhibition assay | Inhibition of human HAL-01 cell growth in a cell viability assay, IC50=1.30175 μM | SANGER | ||
| human NCI-H650 cel | Growth inhibition assay | Inhibition of human NCI-H650 cell growth in a cell viability assay, IC50=1.30076 μM | SANGER | ||
| human NKM-1 cell | Growth inhibition assay | Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=1.28636 μM | SANGER | ||
| human MEL-HO cell | Growth inhibition assay | Inhibition of human MEL-HO cell growth in a cell viability assay, IC50=1.24238 μM | SANGER | ||
| human NCI-H1048 cell | Growth inhibition assay | Inhibition of human NCI-H1048 cell growth in a cell viability assay, IC50=1.22579 μM | SANGER | ||
| human SK-OV-3 cell | Growth inhibition assay | Inhibition of human SK-OV-3 cell growth in a cell viability assay, IC50=1.20444 μM | SANGER | ||
| human CAMA-1 cell | Growth inhibition assay | Inhibition of human CAMA-1 cell growth in a cell viability assay, IC50=1.2001 μM | SANGER | ||
| human HGC-27 cell | Growth inhibition assay | Inhibition of human HGC-27 cell growth in a cell viability assay， IC50=1.1816 μM | SANGER | ||
| human P30-OHK cell | Growth inhibition assay | Inhibition of human P30-OHK cell growth in a cell viability assay, IC50=1.07138 μM | SANGER | ||
| human Daudi cell | Growth inhibition assay | Inhibition of human Daudi cell growth in a cell viability assay, IC50=1.06888 μM | SANGER | ||
| human A427 cell | Growth inhibition assay | Inhibition of human A427 cell growth in a cell viability assay, IC50=0.99505 μM | SANGER | ||
| human HH cell | Growth inhibition assay | Inhibition of human HH cell growth in a cell viability assay, IC50=0.96222 μM | SANGER | ||
| human EW-7 cell | Growth inhibition assay | Inhibition of human EW-7 cell growth in a cell viability assay, IC50=0.86356 μM | SANGER | ||
| human SCC-9 cell | Growth inhibition assay | Inhibition of human SCC-9 cell growth in a cell viability assay, IC50=0.8577 μM | SANGER | ||
| human NCI-H2342 cell | Growth inhibition assay | Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=0.84294 μM | SANGER | ||
| human ES7 cell | Growth inhibition assay | Inhibition of human ES7 cell growth in a cell viability assay, IC50=0.81286 μM | SANGER | ||
| human SK-MES-1 cell | Growth inhibition assay | Inhibition of human SK-MES-1 cell growth in a cell viability assay, IC50=0.78967 μM | SANGER | ||
| human RS4-11 cell | Growth inhibition assay | Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=0.73806 μM | SANGER | ||
| human NALM-6 cell | Growth inhibition assay | Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=0.70465 μM | SANGER | ||
| human OVCAR-3 cell | Growth inhibition assay | Inhibition of human OVCAR-3 cell growth in a cell viability assay, IC50=0.67946 μM | SANGER | ||
| human RPMI-6666 cell | Growth inhibition assay | Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50=0.64379 μM | SANGER | ||
| human OS-RC-2 cell | Growth inhibition assay | Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50=0.62388 μM | SANGER | ||
| human BT-20 cell | Growth inhibition assay | Inhibition of human BT-20 cell growth in a cell viability assay, IC50=0.59222 μM | SANGER | ||
| human SU-DHL-1 cell | Growth inhibition assay | Inhibition of human SU-DHL-1 cell growth in a cell viability assay, IC50=0.56813 μM | SANGER | ||
| human T47D cell | Growth inhibition assay | Inhibition of human T47D cell growth in a cell viability assay, IC50=0.5327 μM | SANGER | ||
| human SW1710 cell | Growth inhibition assay | Inhibition of human SW1710 cell growth in a cell viability assay, IC50=0.5292 μM | SANGER | ||
| human J82 cell | Growth inhibition assay | Inhibition of human J82 cell growth in a cell viability assay, IC50=0.47779 μM | SANGER | ||
| human MDA-MB-415 cell | Growth inhibition assay | Inhibition of human MDA-MB-415 cell growth in a cell viability assay, IC50=0.16732 μM | SANGER | ||
| human VMRC-RCZ cell | Growth inhibition assay | Inhibition of human VMRC-RCZ cell growth in a cell viability assay, IC50=0.14898 μM | SANGER | ||
| human YT cell | Growth inhibition assay | Inhibition of human YT cell growth in a cell viability assay, IC50=0.12066 μM | SANGER | ||
| human A498 cell | Growth inhibition assay | Inhibition of human A498 cell growth in a cell viability assay, IC50=0.11795 μM | SANGER | ||
| human KURAMOCHI cell | Growth inhibition assay | Inhibition of human KURAMOCHI cell growth in a cell viability assay, IC50=0.1051 μM | SANGER | ||
| human SW982 cell | Growth inhibition assay | Inhibition of human SW982 cell growth in a cell viability assay, IC50=0.03584 μM | SANGER | ||
| human RXF393 cell | Growth inhibition assay | Inhibition of human RXF393 cell growth in a cell viability assay, IC50=0.01154 μM | SANGER | ||
| 他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい | |||||
生物活性
| 製品説明 | AZD6482 (KIN-193) is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ in cell-free assays. Phase 1. | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Targets |
|
| In Vitro | ||||
| In vitro | AZD6482 also inhibits PI3Kα, γ, and δ, with IC50 of 80 nM to 1.09 μM, which are significantly lower than its (+)-enantiomer (S-form). AZD6482 is an antiplatelet agent; it blocks platelet activation adhesion/aggregation and promotes platelet disaggregation in assay of washed platelet aggregation (WPA), with an IC50 value of 6 nM. Furthermore, by targeting PI3Kβ, AZD6482 specifically inhibits thrombosis without interfering with normal haemostasis. Therefore, AZD6482 is used as an anti-thrombotic drug for the prophylaxis of thrombotic disorders. [1] | |||
|---|---|---|---|---|
| Kinase Assay | Assay of PI3K enzyme inhibition | |||
| The inhibition of PI3Kβ, PI3Kα, PI3Kγ, and PI3Kδ is evaluated in an AlphaScreen based enzyme activity assay using human recombinant enzymes. The assay measures PI3K-mediated conversion of PIP2 to PIP3. Biotinylated PIP3, a GST-tagged pleckstrin homology (PH) domain and the two AlphaScreen beads form a complex that elicits a signal upon laser excitation at 680 nm. The PIP3 formed in the enzyme reaction competes with the biotinylated PIP3 for binding to the PH domain thus reducing the signal with increasing enzyme product. The AZD6482 is dissolved in DMSO and added to 384 well plates. PBKβ, PBKα, PBKγ, or PBKδ is added in a Tris buffer (50 mM Tris pH 7.6, 0.05% CHAPS, 5 mM DTT, and 24 mM MgCl2) and allowed to preincubate with AZD6482 for 20 minutes prior to the addition of substrate solution containing PIP2 and ATP. The enzyme reaction is stopped after 20 minutes by addition of stop solution containing EDTA and biotin-PIP3, followed by addition of detection solution containing GST-grpl PH and AlphaScreen beads. Plates are left for a minimum of 5 hours in the dark prior to analysis. The final concentration of DMSO, ATP and PIP2 in the assay are, 0.8%, 4 μM, and 40 μM, respectively. IC50 values are calculated according to the equation, y = {a+[(b-a)/(l+(x/IC50)s)]}, where y = % inhibition; a = 0%; b = 100%; s = the slope of the concentration-response curve; x = AZD6482 concentration. | ||||
| 細胞実験 | 細胞株 | Human platelet pellet | ||
| 濃度 | 0–60 nM, dissolved in DMSO | |||
| 反応時間 | 5 min | |||
| 実験の流れ | For assay of washed platelet aggregation (WPA), the platelet pellets are isolated from human blood and re-suspended to 2 × 1015/L in Tyrodes buffer (TB) containing 1 μM hirudin and 0.02 U/mL apyrase. Then, the platelet suspension is left to rest at room temperature for 30 min. Just prior to time for assay, CaCl2 is added to a final concentration of 2 mM. AZD6482, dissolved in DMSO, is added to a 96-well plate prior to the addition of the washed platelet suspension. The platelet suspension is preincubated with AZD6482 for 5 min. Light absorption at 650 nm is recorded before and after a 5 min plate shake and referred to as recording 0 (R0) and Rl. A mouse anti-human CD9 antibody is added (at a donor specific concentration) to each well prior to next 10 min plate shake and light absorption recording; R2. For data analysis, light absorbance in wells with TB are subtracted from all readings before percent aggregation is calculated according the formula: [(R1-R2)/R1] × 100 = % aggregation. Spontaneous aggregation or pro-aggregatory effect of the inhibitor is evaluated by the same formula, [(R0-Rl)/R0] × 100 = % aggregation. IC50 values are calculated according to the equation, y = {a+[(b-a)/(l+(x/IC50)s)]}, where y = % inhibition; a = 0%; b = 100%; s = the slope of the concentration-response curve; x = AZD6482 concentration. | |||
化学情報
| 分子量 | 408.45 | 化学式 | C22H24N4O4 |
| CAS No. | 1173900-33-8 | SDF | Download AZD6482 SDFをダウンロードする |
| Smiles | CC1=CN2C(=O)C=C(N=C2C(=C1)C(C)NC3=CC=CC=C3C(=O)O)N4CCOCC4 | ||
| 保管 | |||
|
In vitro |
DMSO : 82 mg/mL ( (200.75 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 : 10 mg/mL Water : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
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
匹
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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