AZD6482
别名: KIN-193
AZD6482 (KIN-193) 是一种PI3Kβ抑制剂，无细胞试验中IC50为10 nM，作用于PI3Kβ比作用于PI3Kδ， PI3Kα和PI3Kγ选择性分别高8，87和109倍。Phase 1。
AZD6482 Chemical Structure
CAS: 1173900-33-8
客户使用Selleck的AZD6482发表文献24篇
客户使用该产品的4个实验数据
产品质控
AZD6482相关产品
| 相关靶点 | p110α p110β p110δ p110γ C2β Vps34 | 点击展开 |
|---|---|---|
| 相关化合物库 | 激酶抑制剂库 PI3K/Akt 抑制剂库 凋亡分子化合物库 细胞周期化合物库 NF-κB信号通路库 | 点击展开 |
相关信号通路图
PI3K抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | AZD6482 (KIN-193) 是一种PI3Kβ抑制剂，无细胞试验中IC50为10 nM，作用于PI3Kβ比作用于PI3Kδ， PI3Kα和PI3Kγ选择性分别高8，87和109倍。Phase 1。 | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 特性 | AZD6482是PI3Kβ抑制剂，作为抗血小板和抗血栓的药剂。 | ||||||||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | AZD6482是PI3Kβ抑制剂，IC50为21 nM, 然而, AZD6482也抑制PI3Kα,γ,和δ, IC50为 80 nM到1.4 μM, 明显比其(+)-对印异构体(S型)低很多。AZD6482是抗血小板药，在洗涤血小板聚集(WPA)实验中，抑制活化血小板粘附/聚集，且促进血小板解聚，IC50为6 nM。而且, AZD6482靶向作用于PI3Kβ，特定抑制血栓形成而不影响正常止血。因此, AZD6482作为抗血栓药，用于预防血栓疾病。[1] | |||
|---|---|---|---|---|
| 激酶实验 | 抑制PI3K酶实验 | |||
| 通过AlphaScreen酶活性测定使用人重组酶测定对PI3Kβ, PI3Kα, PI3Kγ和 PI3Kδ的抑制效果。该法测量PI3K调节的PIP2和PIP3之间的转换。生物素化的PIP3，即GST-标记的血小板-白细胞C 激酶底物同源(PH) 域和两个AlphaScreen 磁珠形成复合体，在680 nm处形成激光信号。在酶反应复合体中形成的PIP3与生物素化的 PIP3竞争性地结合到PH 域，引起提高酶产物，降低信号。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 预温育20分钟，然后加入含 PIP2和ATP的底物溶液。20分钟后，加入含EDTA 和生物素-PIP3的终止液，而终止酶反应,随后加入含GST-grpl PH 和AlphaScreen磁珠的检测液。实验板在暗中放置最少5小时，然后用于实验分析。实验中DMSO, ATP和 PIP2 的最终浓度分别为0.8%, 4 μM, 和40 μM。计算IC50值。 | ||||
| 细胞实验 | 细胞系 | 人血小板颗粒 | ||
| 浓度 | 0-60 nM, 溶于 DMSO | |||
| 孵育时间 | 5分钟 | |||
| 方法 | 在洗涤血小板聚集 (WPA)实验中,从人血液中分离血小板颗粒，再悬浮在含1 μM水蛭素和0.02 U/mL三磷酸腺苷双磷酸酶的2×1015/L Tyrodes buffer 中。然后，血小板悬浮液在室温下搁置30分钟。实验开始前，加入CaCl2，终浓度为2 mM。AZD6482, 溶于DMSO,加到96孔板中，然后 加入洗涤的血小板悬液。血小板悬液和 AZD6482预温育5分钟。在650 nm处记录吸光值，然后震荡板5分钟再记录吸光值，记为R0和Rl。每孔加入特定浓度的小鼠 抗人CD9抗体 ，震荡板10分钟，记录吸光值，记为R2。用于数据分析, 除去所有数据中和TB结合而测定的吸光值，然后根据公式: [(R1-R2)/R1]×100 计算聚集百分数。另外，根据同样公式 [(R0-Rl)/R0]×100 评定抑制剂的自发聚集效果。然后测定IC50值。 | |||
化学信息&溶解度
| 分子量 | 408.45 | 分子式 | C22H24N4O4 |
| CAS号 | 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 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 82 mg/mL ( (200.75 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 10 mg/mL Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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