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- CAS号：
1402608-02-9
- 规格：
1mLx10mM(inDMSO)/1mg/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥1000.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥394.0 |
| 规格： | 5mg | 产品价格： | ￥904.0 |
| 规格： | 10mg | 产品价格： | ￥1296.0 |
| 规格： | 25mg | 产品价格： | ￥2208.0 |
| 规格： | 50mg | 产品价格： | ￥3096.0 |
| 规格： | 100mg | 产品价格： | ￥4416.0 |
Product Introduction
Bioactivity
| 名称 | BAY1125976 |
| 描述 | BAY1125976 is an allosteric inhibitor of Akt1 and Akt2 (IC50s of 5.2 and 18 nM, respectively, in a time-resolved FRET assay) |
| 激酶实验 | The inhibition of five different recombinant AKT proteins (AKT1, ΔPH‐AKT1, AKT2, ΔPH‐AKT2 and AKT3) by BAY 1125976 was assessed by TR‐FRET‐based in vitro kinase assays, which quantify the phosphorylation of the biotinylated peptide biotin‐Ahx‐KKLNRTLSFAEPG (C‐terminus in amide form) by a recombinant kinase enzyme. The ability of BAY 1125976 to inhibit T308 phosphorylation in inactive AKT1 by the upstream kinase PDK1 was measured by a TR‐FRET‐based in vitro kinase assay. To further characterize the interaction of BAY 1125976 with human full‐length active AKT1 and inactive AKT1, as well as a variant lacking the PH domain, surface plasmon resonance spectroscopy (SPR) was performed by a Biacore T100 instrument. |
| 动物实验 | Female NMRI (nu/nu) mice s.c. injected with 3 × 10^6/100 μl KPL‐4 breast cancer cells were used to study the mode‐of‐action of BAY 1125976. The treatment was started when tumors reached 232–358 mm^3 in size and the mice received a single oral dose of 25 or 50 mg/kg BAY 1125976. For determination of plasma concentration‐time profiles, blood was drawn from the animals at different time points after compound administration. Analysis of the samples was performed on heparinized plasma after precipitation with acetonitrile by LC/MS/MS. Unbound drug concentrations were calculated from total concentrations and the unbound in vitro fraction in plasma was determined by equilibrium analysis. P‐AKT‐S473 levels in tumor tissue extracts were analyzed with a MULTI‐SPOT Assay System/Phospho (Ser473)/Total Akt Whole Cell Lysate Kit from samples taken 2, 5 and 24 hr after compound administration. These lysates were used in addition for analysis of p‐PRAS40‐T246/total‐PRAS40 and AKT signaling (p‐AKT‐S473, p‐GSK3?‐S9, p‐S6RP‐S240/244 and p‐70S6K‐T389) using respective MULTI‐SPOT Assay Systems. Vehicle‐treated tumors were analyzed to determine the basal level of p‐AKT and used to normalize the amount of p‐AKT relative to vehicle levels. |
| 体外活性 | 在体外实验中，BAY1125976抑制了一系列人类癌症细胞系的增殖。尤其是在表达雌激素或雄激素受体的乳腺癌和前列腺癌细胞系中，观察到了较高的活性。 |
| 体内活性 | BAY1125976在活体内对包括KPL4乳腺癌模型（PIK3CAH1074R突变体）、MCF7和HBCx-2乳腺癌模型以及AKTE17K突变驱动的前列腺癌（LAPC-4）和肛门癌（AXF 984）模型等细胞系和患者来源的异种移植模型表现出强效的治疗效果。表明BAY 1125976是一种针对展示PI3K/AKT/mTOR途径激活的肿瘤的强效且高度选择性的AKT1/2异构体抑制剂，为临床开发新的有效治疗提供了机会。 |
| 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+90% Saline : < 2.5 mg/mL (6.52 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2.5 mg/mL (6.52 mM), Solution. DMSO : 25 mg/mL (65.2 mM), Sonication is recommended. |
| 关键字 | Protein kinase B | PKB | Inhibitor | inhibit | BAY-1125976 | BAY1125976 | BAY 1125976 | Akt |
| 相关产品 | Creatine monohydrate | Musk ketone | Aceglutamide | Chloramphenicol | Hyaluronic acid | L-Valine | Methyl eugenol | Artemisinin | 2,3-Butanediol | Bisphenol A | Ethyl linoleate | Stearamide |
| 相关库 | Inhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Anti-Aging Compound Library | Clinical Compound Library | Glycometabolism Compound Library | Immunology/Inflammation Compound Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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相关实验
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 BAY1125976【1402608-02-9】
￥394 - 4416
