- 抑制劑
- 研究領(lǐng)域
- PI3K/Akt/mTOR信號(hào)通路
- 表觀遺傳
- 甲基化
- 免疫&炎癥
- 酪氨酸蛋白激酶
- 血管生成
- 凋亡
- 自噬
- 內(nèi)質(zhì)網(wǎng)應(yīng)激&UPR響應(yīng)
- JAK/STAT信號(hào)通路
- MAPK信號(hào)通路
- 細(xì)胞骨架
- 細(xì)胞周期
- TGF-beta/Smad信號(hào)通路
- DNA損傷/DNA修復(fù)
- 化合物庫(kù)
- 抗體
- 生物試劑
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實(shí)驗(yàn)
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 細(xì)胞核與細(xì)胞漿蛋白抽提試劑盒
- 免疫磁珠
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲(chǔ)液)
- 磷酸酶抑制劑Cocktail
- 細(xì)胞實(shí)驗(yàn)
- Cell Counting Kit-8 (CCK-8)
- 動(dòng)物實(shí)驗(yàn)
- 鼠尾直接PCR試劑盒(快速基因型鑒定)
- 小鼠CD3+ T細(xì)胞分選試劑盒
- 小鼠CD4+ T細(xì)胞分選試劑盒
- 小鼠CD8+ T細(xì)胞分選試劑盒
- 新產(chǎn)品
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AZD6482
別名: KIN-193
AZD6482 (KIN-193) 是一種PI3Kβ抑制劑，無(wú)細(xì)胞試驗(yàn)中IC50為10 nM，作用于PI3Kβ比作用于PI3Kδ， PI3Kα和PI3Kγ選擇性分別高8，87和109倍。Phase 1。
AZD6482 Chemical Structure
CAS: 1173900-33-8
產(chǎn)品質(zhì)控
批次：
S146202
DMSO]82 mg/mL]false]Ethanol]10 mg/mL]false]Water]Insoluble]false
純度：
99.79%
99.79
AZD6482相關(guān)產(chǎn)品
相關(guān)信號(hào)通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)信息(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 | |||
| 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 | |||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | AZD6482 (KIN-193) 是一種PI3Kβ抑制劑，無(wú)細(xì)胞試驗(yàn)中IC50為10 nM，作用于PI3Kβ比作用于PI3Kδ， PI3Kα和PI3Kγ選擇性分別高8，87和109倍。Phase 1。 | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 特性 | AZD6482是PI3Kβ抑制劑，作為抗血小板和抗血栓的藥劑。 | ||||||||
| 靶點(diǎn) |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | AZD6482是PI3Kβ抑制劑，IC50為21 nM, 然而, AZD6482也抑制PI3Kα,γ,和δ, IC50為 80 nM到1.4 μM, 明顯比其(+)-對(duì)印異構(gòu)體(S型)低很多。AZD6482是抗血小板藥，在洗滌血小板聚集(WPA)實(shí)驗(yàn)中，抑制活化血小板粘附/聚集，且促進(jìn)血小板解聚，IC50為6 nM。而且, AZD6482靶向作用于PI3Kβ，特定抑制血栓形成而不影響正常止血。因此, AZD6482作為抗血栓藥，用于預(yù)防血栓疾病。[1] | |||
|---|---|---|---|---|
| 激酶實(shí)驗(yàn) | 抑制PI3K酶實(shí)驗(yàn) | |||
| 通過(guò)AlphaScreen酶活性測(cè)定使用人重組酶測(cè)定對(duì)PI3Kβ, PI3Kα, PI3Kγ和 PI3Kδ的抑制效果。該法測(cè)量PI3K調(diào)節(jié)的PIP2和PIP3之間的轉(zhuǎn)換。生物素化的PIP3，即GST-標(biāo)記的血小板-白細(xì)胞C 激酶底物同源(PH) 域和兩個(gè)AlphaScreen 磁珠形成復(fù)合體，在680 nm處形成激光信號(hào)。在酶反應(yīng)復(fù)合體中形成的PIP3與生物素化的 PIP3競(jìng)爭(zhēng)性地結(jié)合到PH 域，引起提高酶產(chǎn)物，降低信號(hào)。AZD6482 溶于DMSO，加到385孔板上。PBKβ, PBKα, PBKγ, 或PBKδ加到 Tris buffer(50 mM Tris pH 7.6, 0.05% CHAPS, 5 mM DTT, 和24 mM MgCl2) 中，和AZD6482 預(yù)溫育20分鐘，然后加入含 PIP2和ATP的底物溶液。20分鐘后，加入含EDTA 和生物素-PIP3的終止液，而終止酶反應(yīng),隨后加入含GST-grpl PH 和AlphaScreen磁珠的檢測(cè)液。實(shí)驗(yàn)板在暗中放置最少5小時(shí)，然后用于實(shí)驗(yàn)分析。實(shí)驗(yàn)中DMSO, ATP和 PIP2 的最終濃度分別為0.8%, 4 μM, 和40 μM。計(jì)算IC50值。 | ||||
| 細(xì)胞實(shí)驗(yàn) | 細(xì)胞系 | 人血小板顆粒 | ||
| 濃度 | 0-60 nM, 溶于 DMSO | |||
| 孵育時(shí)間 | 5分鐘 | |||
| 方法 | 在洗滌血小板聚集 (WPA)實(shí)驗(yàn)中,從人血液中分離血小板顆粒，再懸浮在含1 μM水蛭素和0.02 U/mL三磷酸腺苷雙磷酸酶的2×1015/L Tyrodes buffer 中。然后，血小板懸浮液在室溫下擱置30分鐘。實(shí)驗(yàn)開(kāi)始前，加入CaCl2，終濃度為2 mM。AZD6482, 溶于DMSO,加到96孔板中，然后 加入洗滌的血小板懸液。血小板懸液和 AZD6482預(yù)溫育5分鐘。在650 nm處記錄吸光值，然后震蕩板5分鐘再記錄吸光值，記為R0和Rl。每孔加入特定濃度的小鼠 抗人CD9抗體 ，震蕩板10分鐘，記錄吸光值，記為R2。用于數(shù)據(jù)分析, 除去所有數(shù)據(jù)中和TB結(jié)合而測(cè)定的吸光值，然后根據(jù)公式: [(R1-R2)/R1]×100 計(jì)算聚集百分?jǐn)?shù)。另外，根據(jù)同樣公式 [(R0-Rl)/R0]×100 評(píng)定抑制劑的自發(fā)聚集效果。然后測(cè)定IC50值。 | |||
|
化學(xué)信息&溶解度
| 分子量 | 408.45 | 分子式 | C22H24N4O4 |
| CAS號(hào) | 1173900-33-8 | SDF | Download AZD6482 SDF |
| Smiles | CC1=CN2C(=O)C=C(N=C2C(=C1)C(C)NC3=CC=CC=C3C(=O)O)N4CCOCC4 | ||
| 儲(chǔ)存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 82 mg/mL ( (200.75 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO) Ethanol : 10 mg/mL (24.48 mM) Water : Insoluble |
摩爾濃度計(jì)算器 |
|
體內(nèi)溶解配方 現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動(dòng)物體內(nèi)配方計(jì)算器 | |||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）
mg/kg
g
μL
只
第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計(jì)算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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