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BAY1125976

产品编号 T7315 CAS 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。

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BAY1125976, CAS 1402608-02-9

规格	价格/CNY	货期
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 * 10 mM (in DMSO)	￥ 1,390	现货

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选择批次

纯度: 98.87%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

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	Akt3:427 nM (IC50, at 10 μM ATP), Akt2:18 nM (IC50, at 10 μM ATP), Akt1:5.2 nM (IC50, at 10 μM ATP)
体外活性	In vitro, BAY1125976 inhibited cell proliferation in a broad panel of human cancer cell lines. Particularly high activity was observed in breast and prostate cancer cell lines expressing estrogen or androgen receptors.
体内活性	BAY1125976 exhibited strong in vivo efficacy in both cell line and patient-derived xenograft models such as the KPL4 breast cancer model (PIK3CAH1074R mutant), the MCF7 and HBCx-2 breast cancer models and the AKTE17K mutant driven prostate cancer (LAPC-4) and anal cancer (AXF 984) models. Indicate that BAY 1125976 is a potent and highly selective allosteric AKT1/2 inhibitor that targets tumors displaying PI3K/AKT/mTOR pathway activation, providing opportunities for the clinical development of new, effective treatments.
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.

分子量	383.45
分子式	C23H21N5O
CAS No.	1402608-02-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 10.33 mg/mL (26.94 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6079 mL	13.0395 mL	26.079 mL	65.1975 mL
	5 mM	0.5216 mL	2.6079 mL	5.2158 mL	13.0395 mL
	10 mM	0.2608 mL	1.304 mL	2.6079 mL	6.5198 mL
	20 mM	0.1304 mL	0.652 mL	1.304 mL	3.2599 mL

计算器

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参考文献

1. Politz O , Siegel F , Bärfacker L, et al. BAY 1125976, a selective allosteric AKT1/2 inhibitor exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models[J]. International Journal of Cancer, 2016, 140(2):449-459.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

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：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 μL，一共给药动物10 只，您使用的配方为5% 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 μL DMSO (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：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：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。

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计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

BAY1125976 1402608-02-9 Cytoskeletal Signaling PI3K/Akt/mTOR signaling Akt inhibit Inhibitor Protein kinase B BAY 1125976 PKB BAY-1125976 inhibitor

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BAY1125976

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

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剂量换算

体内实验配液计算器

技术支持

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