化合物 BAY1125976|T7315|TargetMol

價(jià)格	￥678	￥980	￥1650
包裝	1mg	2mg	5mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-12

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產(chǎn)品詳情

中文名稱:化合物 BAY1125976	英文名稱:BAY1125976
CAS:1402608-02-9	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: ≥98%	產(chǎn)品類別: 抑制劑
貨號(hào): T7315

Product Introduction

Bioactivity

名稱	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)
激酶實(shí)驗(yàn)	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.
動(dòng)物實(shí)驗(yàn)	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.
體外活性	在體外實(shí)驗(yàn)中，BAY1125976抑制了一系列人類癌癥細(xì)胞系的增殖。尤其是在表達(dá)雌激素或雄激素受體的乳腺癌和前列腺癌細(xì)胞系中，觀察到了較高的活性。
體內(nèi)活性	BAY1125976在活體內(nèi)對(duì)包括KPL4乳腺癌模型（PIK3CAH1074R突變體）、MCF7和HBCx-2乳腺癌模型以及AKTE17K突變驅(qū)動(dòng)的前列腺癌（LAPC-4）和肛門癌（AXF 984）模型等細(xì)胞系和患者來(lái)源的異種移植模型表現(xiàn)出強(qiáng)效的治療效果。表明BAY 1125976是一種針對(duì)展示PI3K/AKT/mTOR途徑激活的腫瘤的強(qiáng)效且高度選擇性的AKT1/2異構(gòu)體抑制劑，為臨床開發(fā)新的有效治療提供了機(jī)會(huì)。
存儲(chǔ)條件	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.
關(guān)鍵字	inhibit \| Inhibitor \| Protein kinase B \| Akt \| BAY1125976 \| BAY 1125976 \| PKB \| BAY-1125976
相關(guān)產(chǎn)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
相關(guān)庫(kù)	抑制劑庫(kù) \| 經(jīng)典已知活性庫(kù) \| 抗癌活性化合物庫(kù) \| 已知活性化合物庫(kù) \| 激酶抑制劑庫(kù) \| 抗衰老化合物庫(kù) \| NO PAINS 化合物庫(kù) \| 藥物功能重定位化合物庫(kù) \| 抗癌臨床化合物庫(kù) \| 抗癌藥物庫(kù)

關(guān)鍵字： BAY1125976|TargetMol

公司簡(jiǎn)介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)國(guó)家和地區(qū)，已發(fā)展成為全球知名的化合物庫(kù)和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫(kù)，以及多種類型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)三大技術(shù)中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

成立日期	2013-04-18 （12年）	注冊(cè)資本	566.265100萬(wàn)人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營(yíng)行業(yè)	天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù)	經(jīng)營(yíng)模式	貿(mào)易,工廠,試劑,定制,服務(wù)

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公司成立：12年
注冊(cè)資本：566.265100萬(wàn)人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營(yíng)產(chǎn)品：小分子抑制劑、藥物篩選化合物庫(kù)、藥物篩選等
公司地址：靜安區(qū)江場(chǎng)三路238號(hào)8樓

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