化合物 666-15|T5318|TargetMol

價(jià)格	￥413	￥945	￥1530
包裝	1mg	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 666-15	英文名稱:666-15
CAS:1433286-70-4	品牌: TargetMol
產(chǎn)地: 美國	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: 99.77%	產(chǎn)品類別: 抑制劑
貨號: T5318

Product Introduction

Bioactivity

名稱	666-15
描述	666-15 is a selective CREB inhibitor with an IC50 of 81 nM. 666-15 can effectively inhibit the growth of breast cancer.
細(xì)胞實(shí)驗(yàn)	HEK 293T cells in a 10 cm plate were transfected with pCRE-RLuc (6 μg) with Lipofectamine2000 following the manufacturer's instructions. Three hours after transfection, the cells were collected and replated into 96-well plates at ～10?000 cells/well. The cells were allowed to attach to the bottom of the plates overnight. The cells were then treated with different concentrations of different compounds for 30 min when forskolin (10 μM) was added to each well. The cells were incubated for further 5 h before cell lysis using 1× 30 μL Renilla luciferase lysis buffer. An amount of 5 μL of the lysate was combined with 30 μL of benzyl-coelenterazine solution in PBS (pH 7.4, 10 μg/mL). The protein concentration in each well was determined. The Renilla luciferase activity was normalized to protein content in each well and expressed as relative luciferase unit/μg protein (RLU/μg protein). The IC50 was derived from nonlinear regression analysis of the RLU/μg protein–concentration curve [1].
動(dòng)物實(shí)驗(yàn)	Each 6- to 8-week old BALB/c nude mouse was inoculated subcutaneously at the right flank with MDA-MB-468 cells (5 × 10^6) in 0.1 mL of HBSS with Matrigel (1:1) for tumor development. When the tumor volume reached approximately 100 mm3, the mice were randomized to be treated with either vehicle or 666-15 at 10 mg/kg. 3i was dissolved in 1% N-methylpyrrolidone (NMP), 5% Tween-80 in H2O. The dosing solution was prepared weekly. The mice were treated once a day for 5 consecutive days a week, and the treatment lasted for 5 weeks. During the treatment, the tumor size and body weight were measured 2–3 times a week. The tumors were measured in two dimensions using a digital caliper, and the volume was expressed in mm3 using the formula V = 0.5ab2, where a and b represent the long and short diameters of the tumor, respectively. The tumor volume was normalized to the initial tumor volume at the time of the first treatment [1].
體外活性	方法：666-15濃度為62.5至500nM處理OA 樣軟骨細(xì)胞，研究 666-15 對 OA 樣老年豚鼠軟骨細(xì)胞的活力。結(jié)果：p-CREB1蛋白水平顯著降低，并顯著提高老年豚鼠軟骨細(xì)胞的細(xì)胞活力。[1] 方法：為了研究CREB抑制的生物學(xué)效應(yīng)，將SySa細(xì)胞與濃度增加（0.13-5μM）的666-15一起孵育并進(jìn)行在MTT測定。結(jié)果：666-15以劑量依賴性方式顯著抑制SySa細(xì)胞活力（IC50：0.36-1.72 μM）。[2]
體內(nèi)活性	方法：小鼠被隨機(jī)分配到不同組別，包括正常組、假手術(shù)組、ACLT+溶劑對照組、以及兩個(gè)不同劑量的666-15處理組（ACLT+666-15低劑量組，5 mg/kg；ACLT+666-15高劑量組，10 mg/kg,腹腔注射，每周一次，六周）。結(jié)果：666-15治療能緩解關(guān)節(jié)退變，降低軟骨中降解標(biāo)志物如CTX-II的水平，減輕滑膜炎癥，且不影響小鼠體重，表明其安全性。[1]
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 : 60 mg/mL (96.7 mM)
關(guān)鍵字	breast \| Epigenetic Reader Domain \| cancer \| CREB \| 66615 \| 666-15 \| 666 15 \| inhibit \| Inhibitor
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關(guān)鍵字： CREB inhibitor|TargetMol

公司簡介

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)國家和地區(qū)，已發(fā)展成為全球知名的化合物庫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，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）	注冊資本	566.265100萬人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營行業(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
注冊資本：566.265100萬人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營產(chǎn)品：小分子抑制劑、藥物篩選化合物庫、藥物篩選等
公司地址：靜安區(qū)江場三路238號8樓

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