AZD6482

別名：KIN-193

製品コード：S1462 純度：99.79%

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

サイズ	価格(税別)	在庫状況
5mg	JPY 25500	国内在庫あり
10mg	JPY 48000	国内在庫あり
50mg	JPY 145500	国内在庫あり

代表番号: 045-509-1970\|電子メール：sales@selleck.co.jp よく尋ねられる質問

文献中Selleckの製品使用例（27）

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製品安全説明書

現在のバッチを見る： S146202 DMSO] 82 mg/mL] false] Ethanol] 10 mg/mL] false] Water] Insoluble] false 純度： 99.79%

99.79

AZD6482関連製品

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関連化合物ライブラリー	Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library	もっと見る

シグナル伝達経路

PI3Kシグナル伝達経路

PI3K阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	活性情報
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
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
human NCI-H1755 cell	Growth inhibition assay	Inhibition of human NCI-H1755 cell growth in a cell viability assay, IC50=3.27063 μM
human NCI-H2030 cell	Growth inhibition assay	Inhibition of human NCI-H2030 cell growth in a cell viability assay, IC50=2.90288 μM
human SF295 cell	Growth inhibition assay	Inhibition of human SF295 cell growth in a cell viability assay, IC50=2.76955 μM
human SW1088 cell	Growth inhibition assay	Inhibition of human SW1088 cell growth in a cell viability assay, IC50=2.48143 μM
human GDM-1 cell	Growth inhibition assay	Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=2.24206 μM
human COLO-684 cell	Growth inhibition assay	Inhibition of human COLO-684 cell growth in a cell viability assay, IC50=2.20032 μM
human D-542MG cell	Growth inhibition assay	Inhibition of human D-542MG cell growth in a cell viability assay, IC50=1.85077 μM
human HSC-2 cell	Growth inhibition assay	Inhibition of human HSC-2 cell growth in a cell viability assay, IC50=1.75727 μM
human EB2 cell	Growth inhibition assay	Inhibition of human EB2 cell growth in a cell viability assay, IC50=1.75019 μM
human LoVo cell	Growth inhibition assay	Inhibition of human LoVo cell growth in a cell viability assay, IC50=1.73825 μM
human D-336MG cell	Growth inhibition assay	Inhibition of human D-336MG cell growth in a cell viability assay, IC50=1.6688 μM
human SNB75 cell	Growth inhibition assay	Inhibition of human SNB75 cell growth in a cell viability assay, IC50=1.66508 μM
human HCC70 cell	Growth inhibition assay	Inhibition of human HCC70 cell growth in a cell viability assay, IC50=1.66146 μM
human 639-V cell	Growth inhibition assay	Inhibition of human 639-V cell growth in a cell viability assay, IC50=1.63144 μM
human HuO9 cell	Growth inhibition assay	Inhibition of human HuO9 cell growth in a cell viability assay, IC50=1.6128 μM
human KU812 cell	Growth inhibition assay	Inhibition of human KU812 cell growth in a cell viability assay, IC50=1.59628 μM
human OCUB-M cell	Growth inhibition assay	Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=1.58314 μM
human NCI-H2291 cell	Growth inhibition assay	Inhibition of human NCI-H2291 cell growth in a cell viability assay, IC50=1.5761 μM
human SNU-423 cell	Growth inhibition assay	Inhibition of human SNU-423 cell growth in a cell viability assay, IC50=1.57192 μM
human MFE-296 cell	Growth inhibition assay	Inhibition of human MFE-296 cell growth in a cell viability assay, IC50=1.56836 μM
human LXF-289 cell	Growth inhibition assay	Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=1.55104 μM
human NB12 cell	Growth inhibition assay	Inhibition of human NB12 cell growth in a cell viability assay, IC50=1.54842 μM
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
human MC116 cell	Growth inhibition assay	Inhibition of human MC116 cell growth in a cell viability assay, IC50=1.46122 μM
human CCF-STTG1 cell	Growth inhibition assay	Inhibition of human CCF-STTG1 cell growth in a cell viability assay, IC50=1.42525 μM
human Becker cell	Growth inhibition assay	Inhibition of human Becker cell growth in a cell viability assay, IC50=1.36315 μM
human GI-1 cell	Growth inhibition assay	Inhibition of human GI-1 cell growth in a cell viability assay, IC50=1.31808 μM
human 786-0 cell	Growth inhibition assay	Inhibition of human 786-0 cell growth in a cell viability assay, IC50=1.31283 μM
human HAL-01 cell	Growth inhibition assay	Inhibition of human HAL-01 cell growth in a cell viability assay, IC50=1.30175 μM
human NCI-H650 cel	Growth inhibition assay	Inhibition of human NCI-H650 cell growth in a cell viability assay, IC50=1.30076 μM
human NKM-1 cell	Growth inhibition assay	Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=1.28636 μM
human MEL-HO cell	Growth inhibition assay	Inhibition of human MEL-HO cell growth in a cell viability assay, IC50=1.24238 μM
human NCI-H1048 cell	Growth inhibition assay	Inhibition of human NCI-H1048 cell growth in a cell viability assay, IC50=1.22579 μM
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
human CAMA-1 cell	Growth inhibition assay	Inhibition of human CAMA-1 cell growth in a cell viability assay, IC50=1.2001 μM
human HGC-27 cell	Growth inhibition assay	Inhibition of human HGC-27 cell growth in a cell viability assay， IC50=1.1816 μM
human P30-OHK cell	Growth inhibition assay	Inhibition of human P30-OHK cell growth in a cell viability assay, IC50=1.07138 μM
human Daudi cell	Growth inhibition assay	Inhibition of human Daudi cell growth in a cell viability assay, IC50=1.06888 μM
human A427 cell	Growth inhibition assay	Inhibition of human A427 cell growth in a cell viability assay, IC50=0.99505 μM
human HH cell	Growth inhibition assay	Inhibition of human HH cell growth in a cell viability assay, IC50=0.96222 μM
human EW-7 cell	Growth inhibition assay	Inhibition of human EW-7 cell growth in a cell viability assay, IC50=0.86356 μM
human SCC-9 cell	Growth inhibition assay	Inhibition of human SCC-9 cell growth in a cell viability assay, IC50=0.8577 μM
human NCI-H2342 cell	Growth inhibition assay	Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=0.84294 μM
human ES7 cell	Growth inhibition assay	Inhibition of human ES7 cell growth in a cell viability assay, IC50=0.81286 μM
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
human RS4-11 cell	Growth inhibition assay	Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=0.73806 μM
human NALM-6 cell	Growth inhibition assay	Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=0.70465 μM
human OVCAR-3 cell	Growth inhibition assay	Inhibition of human OVCAR-3 cell growth in a cell viability assay, IC50=0.67946 μM
human RPMI-6666 cell	Growth inhibition assay	Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50=0.64379 μM
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
human BT-20 cell	Growth inhibition assay	Inhibition of human BT-20 cell growth in a cell viability assay, IC50=0.59222 μM
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
human T47D cell	Growth inhibition assay	Inhibition of human T47D cell growth in a cell viability assay, IC50=0.5327 μM
human SW1710 cell	Growth inhibition assay	Inhibition of human SW1710 cell growth in a cell viability assay, IC50=0.5292 μM
human J82 cell	Growth inhibition assay	Inhibition of human J82 cell growth in a cell viability assay, IC50=0.47779 μM
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
human VMRC-RCZ cell	Growth inhibition assay	Inhibition of human VMRC-RCZ cell growth in a cell viability assay, IC50=0.14898 μM
human YT cell	Growth inhibition assay	Inhibition of human YT cell growth in a cell viability assay, IC50=0.12066 μM
human A498 cell	Growth inhibition assay	Inhibition of human A498 cell growth in a cell viability assay, IC50=0.11795 μM
human KURAMOCHI cell	Growth inhibition assay	Inhibition of human KURAMOCHI cell growth in a cell viability assay, IC50=0.1051 μM
human SW982 cell	Growth inhibition assay	Inhibition of human SW982 cell growth in a cell viability assay, IC50=0.03584 μM
human RXF393 cell	Growth inhibition assay	Inhibition of human RXF393 cell growth in a cell viability assay, IC50=0.01154 μM
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

PI3Kβ ^[1] (Cell-free assay)	PI3Kδ ^[1] (Cell-free assay)	DNA-PK ^[1] (Cell-free assay)	PI3Kα ^[1] (Cell-free assay)
10 nM	80 nM	420 nM	870 nM

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). This compound 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, this chemical specifically inhibits thrombosis without interfering with normal haemostasis. Therefore, it is used as an anti-thrombotic drug for the prophylaxis of thrombotic disorders. ^[1]
Kinase Assay	Assay of PI3K enzyme inhibition
Kinase Assay	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. This compound 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 this chemical 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 = this compound 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 this compound 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 = this chemical concentration.

参考
http://www.wipo.int/patentscope/search/en/WO2009093972

参考

http://www.wipo.int/patentscope/search/en/WO2009093972

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	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

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
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
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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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