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- CAS号：
1173900-33-8
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mg | 产品价格： | ￥285.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥534.0 |
| 规格： | 5mg | 产品价格： | ￥596.0 |
| 规格： | 10mg | 产品价格： | ￥984.0 |
| 规格： | 25mg | 产品价格： | ￥1584.0 |
| 规格： | 50mg | 产品价格： | ￥2984.0 |
| 规格： | 100mg | 产品价格： | ￥4256.0 |
Product Introduction
Bioactivity
| 名称 | AZD 6482 |
| 描述 | AZD 6482 (KIN-193) is a potent and selective inhibitor of p110β and PI3Kβ with IC50 values of 0.69nM and 10nM, respectively. AZD 6482 is particularly effective in blocking AKT signaling and tumor growth dependent on p110β activation or PTEN loss. |
| 细胞实验 | 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. (Only for Reference) |
| 激酶实验 | 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. |
| 体外活性 | 方法：AZD 6482 (KIN-193) （0.625，1.25，2.5，5，10，20 ， 40 μM，48小时）测定处理 U87 和 U118细胞，CCK8测定其对 U87 和 U118 细胞增殖的抑制作用。 结果：AZD 6482以剂量依赖式方式抑制两种细胞系的活力，其中U118 细胞比 U87 细胞更敏感，IC50值分别为 7.989 和 9.061μM。[4] |
| 体内活性 | 方法：AZD 6482 (KIN-193) （20 mg/kg，腹腔注射，每天两次）或 GDC-0941（150 mg/kg，口服，每天一次）处理 HCC70、PC3 和 HCC1954 的异种移植肿瘤小鼠，研究KIN-193 对 PTEN 缺陷肿瘤的体内效应。 结果：AZD 6482 显著抑制 HCC70 和 PC3 肿瘤的肿瘤生长，但未能阻断 HCC1954 肿瘤的生长。[2] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 7.5 mg/mL (18.36 mM), Solution. 10% DMSO+90% Saline : < 7.5 mg/mL (18.36 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. DMSO : 75 mg/mL (183.62 mM), Sonication is recommended. |
| 关键字 | PI3Kδ | PI3Kγ | PI3Kβ | PI3Kα | PI3K | Phosphoinositide 3-kinase | KIN-193 | KIN193 | Inhibitor | inhibit | DNA-PK | DNAPK | AZD-6482 | AZD 6482 | Autophagy |
| 相关产品 | Guanidine hydrochloride | Naringin | Enzalutamide | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Hemin | Hydroxychloroquine | Sildenafil citrate | Stavudine | Tamoxifen | Paeonol |
| 相关库 | Inhibitor Library | Immuno-Oncology Compound Library | Anti-Breast Cancer Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Anti-Aging Compound Library | Antioxidant Compound Library | Immunology/Inflammation Compound Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 AZD6482【1173900-33-8】
￥285 - 4256
