化合物 BAY1125976|T7315|TargetMol

BAY1125976
1402608-02-9

￥678 1mg 起订

￥980 2mg 起订

￥1650 5mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 BAY1125976

英文名称：: BAY1125976

CAS号：: 1402608-02-9

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: ≥98%

产品类别：: 抑制剂

货号：: T7315

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.
溶解度	DMSO : 5 mg/mL (13.04 mM), Sonication is recommended.
关键字	inhibit \| Inhibitor \| Protein kinase B \| Akt \| BAY1125976 \| BAY 1125976 \| PKB \| BAY-1125976
相关产品	(E)-Akt inhibitor-IV \| Honokiol \| Capivasertib \| Methyl-Hesperidin \| AKT Kinase Inhibitor \| Artemisinin \| 2,3-Butanediol \| PI3K/Akt/mTOR-IN-2 \| Oridonin \| Ethyl gallate \| Urolithin B \| SKLB-163
相关库	抑制剂库 \| 经典已知活性库 \| 抗癌活性化合物库 \| 已知活性化合物库 \| 激酶抑制剂库 \| 抗衰老化合物库 \| NO PAINS 化合物库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库 \| 抗癌药物库

BAY1125976|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	(12年)
注册资本	566.265100万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,工厂,试剂,定制,服务
主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务