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BAY1125976

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产品编号 T7315Cas号 1402608-02-9

BAY1125976 是选择性Akt1/Akt2变构抑制剂。在10 μM ATP 时,它抑制 Akt1 和 Akt2 活性的IC50值分别为 5.2 nM 和 18 nM。

BAY1125976
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BAY1125976

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纯度: 98.87%
产品编号 T7315Cas号 1402608-02-9

BAY1125976 是选择性Akt1/Akt2变构抑制剂。在10 μM ATP 时,它抑制 Akt1 和 Akt2 活性的IC50值分别为 5.2 nM 和 18 nM。

规格价格库存数量
1 mg¥ 678现货
2 mg¥ 980现货
5 mg¥ 1,650现货
10 mg¥ 2,320现货
25 mg¥ 4,000现货
50 mg¥ 5,680现货
100 mg¥ 7,950现货
500 mg¥ 15,900现货
1 mL x 10 mM (in DMSO)¥ 1,390现货
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产品介绍

生物活性
产品描述
BAY1125976 is an allosteric inhibitor of Akt1 and Akt2 (IC50s of 5.2 and 18 nM, respectively, in a time-resolved FRET assay)
靶点活性
Akt1:5.2 nM (IC50, at 10 μM ATP), Akt2:18 nM (IC50, at 10 μM ATP), Akt3:427 nM (IC50, at 10 μM ATP)
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。
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.
化学信息
分子量383.45
分子式C23H21N5O
CAS No.1402608-02-9
SmilesNC(=O)c1ccc2nc(c(-c3ccccc3)n2n1)-c1ccc(cc1)C1(N)CCC1
密度no data available
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 5 mg/mL (13.04 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.6079 mL13.0395 mL26.0790 mL130.3951 mL
5 mM0.5216 mL2.6079 mL5.2158 mL26.0790 mL
10 mM0.2608 mL1.3040 mL2.6079 mL13.0395 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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