BET bromodomain inhibitor 1,BET bromodomain inhibitor 1

BET bromodomain inhibitor 1|T39998|TargetMol

價格	￥2120
包裝	2mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-09-30

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產(chǎn)品詳情

中文名稱:BET bromodomain inhibitor 1	英文名稱:BET bromodomain inhibitor 1
CAS:2411226-02-1	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.
產(chǎn)品類別: 抑制劑
貨號: T39998

Product Introduction

Bioactivity

名稱	BET bromodomain inhibitor 1
描述	BET bromodomain inhibitor 1 is an orally active, selective inhibitor of bromodomain and extra-terminal (BET) proteins. It specifically inhibits BRD4 with an IC50 of 2.6 nM. Additionally, BET bromodomain inhibitor 1 demonstrates high affinities towards BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, and 2.1 nM, respectively. This compound exhibits anti-cancer activity.
體外活性	BET bromodomain inhibitor 1 (compound 38; 31.25-125 nM; 24 hours) leads to more pronounced G1-phase cell cycle arrest[1]. BET bromodomain inhibitor 1 (31.25-500 nM; 6 or 24 hours) is highly effective in inducing dose-dependent inhibition on c-Myc expression and upregulation of p21 levels[1]. BET bromodomain inhibitor 1 (31.25-125 nM; 6 hours) robustly reduces the expressions of c-Myc, BCL-2, and CDK6[1]. BET bromodomain inhibitor 1 does not inhibit five cytochrome P450 enzymes (IC 50 >20 μM)[1]. BET bromodomain inhibitor 1 demonstrates an excellent selectivity for the BET bromodomain family over other bromodomains, with an ～1500-fold selectivity for BRD4(1) over EP300 (IC 50 =3857 nM)[1]. BET bromodomain inhibitor 1 strongly inhibited the growth of acute myeloid leukemia cell line MV4-11, acute leukemia cell lines Kasumi-1 and RS-4-11, and multiple myeloma cancer cell line MM1.S cells with IC 50 values of 2.4, 4.8, 17.6 and 15.1 nM, respectively[1]. Cell Cycle Analysis[1]Cell Line: MV-4-11 cells Concentration: 31.25, 62.5, 125 nM Incubation Time: 24 hours Result: Led to more pronounced G1-phase cell cycle arrest. Western Blot Analysis[1]Cell Line: MV-4-11 cells Concentration: 31.25, 62.5, 125, 250, 500 nM Incubation Time: 6 or 24 hours Result: Induced dose-dependent inhibition on c-Myc expression and upregulation of p21 levels. RT-PCR[1]Cell Line: MV-4-11 cells Concentration: 31.25, 62.5, 125 nM Incubation Time: 6 hours Result: Robustly reduced the expressions of c-Myc, BCL-2, and CDK6.
體內(nèi)活性	BET bromodomain inhibitor 1 (compound 38; 6.25, 12.5 mg/kg; PO; daily ; for 28 days) exhibits stronger antitumor activities and completely inhibits the growth of tumor with a tumor growth inhibition (TGI) of 99.7% at 12.5 mg/kg[1]. BET bromodomain inhibitor 1 (1 mg/kg; IV) has a T 1/2 of 1.3 and 0.9 hours, a CL of 21.5 and 15.3 mL/min?kg, and a V ss of 1464 and 782 mL/kg for rats and mouse, respectively[1]. BET bromodomain inhibitor 1 (3 mg/kg; PO) has a T 1/2 of 3.6 hours, a C max of 159 ng/mL and an AUC of 884 ng?h/mL for rats[1]. BET bromodomain inhibitor 1 (1.3 mg/kg; PO) has a T 1/2 of 1.3 hours, a C max of 399 ng/mL and an AUC of 1710 ng?h/mL for mouse[1]. Animal Model: An MV4-11 mouse xenograft model[1]Dosage: 6.25, 12.5 mg/kg Administration: PO; daily ; for 28 days Result: Exhibited stronger antitumor activities and completely inhibited the growth of tumor with a tumor growth inhibition (TGI) of 99.7% at 12.5 mg/kg. Animal Model: Male SD rats[1]Dosage: 1 mg/kg (Pharmacokinetic Analysis) Administration: IV Result: Had a T 1/2 of 1.3 hours, a CL of 21.5 mL/min?kg, and a V ss of 1464 mL/kg.
存儲條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
關鍵字	BET bromodomain inhibitor 1

關鍵字： BET bromodomain inhibitor 1|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域科學家的研究提供專業(yè)的產(chǎn)品和服務。TargetMol?品牌的客戶群分布于40多個國家和地區(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、生命科學試劑盒等，此外，我們還建設有CADD（計算機輔助藥物設計）研究中心、藥理實驗室、藥化合成平臺三大技術中心，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、快速高效的全球供應鏈和專業(yè)的技術支持，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	年營業(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,分子砌塊,生物技術服務	經(jīng)營模式	貿(mào)易,工廠,試劑,定制,服務

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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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BET bromodomain inhibitor 1|T39998|TargetMol相關廠家報價

產(chǎn)品名稱	價格		公司名稱	報價日期
BET bromodomain抑制劑(GSK525762A)	詢價	VIP5年	上海澤葉生物科技有限公司	2024-11-15
MS436 (BET Bromodomain抑制劑)	詢價		碧云天生物技術有限公司	2024-11-05
I-BET 151	詢價	VIP8年	上海瀚香生物科技有限公司	2024-11-15

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