化合物 Y06036|T5362|TargetMol

價(jià)格	￥258	￥398	￥663
包裝	2mg	5mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-09-29

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產(chǎn)品詳情

中文名稱:化合物 Y06036	英文名稱:Y06036
CAS:1832671-96-1	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: 98.95%	產(chǎn)品類別: 抑制劑
貨號(hào): T5362

Product Introduction

Bioactivity

名稱	Y06036
描述	Y06036, a potent and selective BET inhibitor, can bind to the BRD4(1) bromodomain (Kd: 82 nM).
細(xì)胞實(shí)驗(yàn)	LNCaP, C4-2B, 22Rv1, and VCaP prostate cancer cells were cultured in RPMI 1640 with 10% FBS at 37 °C and an atmosphere of 5% CO2. For cell viability, cells were seeded in 384-well plates at 500?1000 cells per well (optimum density for growth) in a total volume of 20 μL of media. After 12 h, 10 μL of chemical compounds with 2-fold or 3-fold serial dilution was added to each well with final concentration from 5 nM to 100 μM. The measurement was conducted 96 h after seeded for LNCaP, C4-2B, and 22Rv1 and 144 h after seeded for VCaP. Then, 25 μL of CellTiter-GLO reagents was added, and luminescence was measured on GLOMAX microplate luminometer, according to the manufacturer's instructions. The estimated in vitro half-maximal inhibitory concentration (IC50) values were calculated using Prism 6 software.
動(dòng)物實(shí)驗(yàn)	Four-week-old male mice (strain: C.B-17/IcrHsd-Prkdcscid for C4-2B) were used for tumor inoculation. Each mouse was inoculated subcutaneously at the dorsal flank on both sides of the mice with C4-2B tumor cells (2 × 10^6 cells) in a mixture of 100 μL PBS and Matrigel (1:1). When the tumor volume reached approximately 100 mm3, the mice were randomized into groups (n = 5?7 per group) and then treated intraperitoneally (ip) with 100 μL of either vehicle or Y06036 and 7m (in a formulation of 15% Cremophor EL, Calbiochem, 82.5% PBS, and 2.5% DMSO) five times per week. The length (L) and width (W) of the tumor mass were monitored by calipers, and volume was expressed in mm3 calculated with the equation V = (π/6)(L × W2). Tumor growth inhibition (TGI) was calculated using the equation TGI = [1 ? (T ? T0)/(C ? C0)] × 100, wherein T and T0 are the mean tumor volumes on a specific experimental day and on the first day of treatment, respectively, for the test groups; and likewise C and C0 are the mean tumor volumes for the vehicle group.
體外活性	Y06036與BRD4(1)溴結(jié)構(gòu)域結(jié)合，其Kd值為82 nM。Y06036在前列腺癌細(xì)胞系中強(qiáng)效抑制細(xì)胞增長(zhǎng)、集落形成以及AR、AR調(diào)控基因和MYC的表達(dá)。
體內(nèi)活性	小鼠在腫瘤體積達(dá)到約100 mm3時(shí)，隨機(jī)分組并通過(guò)腹膜內(nèi)(i.p.)給藥，接受安慰劑或BET抑制劑Y06036（50 mg/kg，每周5次）治療。在25天的治療期間，Y06036表現(xiàn)出強(qiáng)大的抗腫瘤活性，腫瘤生長(zhǎng)抑制(TGI)達(dá)到70%。
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 : 100 mg/mL (234 mM)
關(guān)鍵字	inhibit \| Epigenetic Reader Domain \| Y06036 \| Inhibitor \| Y 06036 \| Y-06036
相關(guān)產(chǎn)品	Bisdemethoxycurcumin \| dBET6 \| 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one \| CeMMEC1 \| (+)-JQ-1 \| Curcumin \| Naphthol AS-E \| J-147 \| ABBV-744 \| Piflufolastat \| Hexamethylene bisacetamide \| Anacardic Acid
相關(guān)庫(kù)	抑制劑庫(kù) \| 抗癌活性化合物庫(kù) \| 經(jīng)典已知活性庫(kù) \| 抗癌化合物庫(kù) \| 已知活性化合物庫(kù) \| 組蛋白修飾化合物庫(kù) \| 表觀遺傳庫(kù) \| PPI抑制劑庫(kù)

關(guān)鍵字： Y06036|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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