貨號	規格	價格	上海	北京	武漢	南京
S80242-1mg	99.0%	￥168.00 S80242-1mg ￥168.00 現貨	7 7	-	-	-
S80242-5mg	99.0%	￥320.00 S80242-5mg ￥320.00 現貨	6 6	-	-	-
S80242-10mg	99.0%	￥416.00 S80242-10mg ￥416.00 現貨	4 4	-	-	-
S80242-25mg	99.0%	￥760.00 S80242-25mg ￥760.00 現貨	6 6	-	-	-
S80242-50mg	99.0%	￥1040.00 S80242-50mg ￥1040.00 現貨	4 4	-	-	-
S80242-100mg	99.0%	￥1520.00 S80242-100mg ￥1520.00 現貨	6 6	-	-	-
S80242-500mg	99.0%	￥4800.00 S80242-500mg ￥4800.00 現貨	6 6	-	-	-

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產品介紹

(+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy

產品描述：

(+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy

靶點：

IC50: 77/33 nM (BRD4(1/2));EpigeneticReaderDomain;Autophagy;LigandsforTargetProteinforPROTAC

體內研究：

Matched cohorts of mice with established tumors are randomized to treatment with (+)-JQ1 (50 mg/kg) or vehicle, administered by daily intraperitoneal injection. Prior to randomization, and after four days of therapy, mice are evaluated by FDG-PET imaging. A marked reduction in FDG uptake is observed with (+)-JQ1 treatment. Tumor-volume measurements confirm a reduction in tumor growth with JQ1 treatment. Pharmacokinetic studies of (+)-JQ1 are performed in CD1 mice following intravenous and oral administration. Mean plasma concentration-time profiles of (+)-JQ1 after intravenous dosing (5 mg/kg). The pharmacokinetic parameters for intravenous (+)-JQ1 demonstrate excellent drug exposure (AUC=2090 hr*ng/mL) and an approximately one hour half-life (T1/2). Mean plasma concentration-time profiles of (+)-JQ1 after oral dosing (10 mg/kg). The pharmacokinetic parameters for oral (+)-JQ1 demonstrate excellent oral bioavailability (F=49%), peak plasma concentration (Cmax=1180 ng/mL) and drug exposure (AUC=2090 hr*ng/mL)

參考文獻：

1. Filippakopoulos P, et al. Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73. 2. Sakamaki JI, et al. Bromodomain Protein BRD4 Is a Transcriptional Repressor of Autophagy and LysosomalFunction. Mol Cell. 2017 May 18;66(4):517-532.e9. 3. Matzuk MM, et al. Small-molecule inhibition of BRDT for male contraception. Cell. 2012 Aug 17;150(4):673-84.

溶解性：

DMSO : ≥ 45 mg/mL (98.47 mM)

保存條件：

2-8℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.188 ml	10.941 ml	21.882 ml
5 mM	0.438 ml	2.188 ml	4.376 ml
10 mM	0.219 ml	1.094 ml	2.188 ml
50 mM	0.044 ml	0.219 ml	0.438 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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(+)-JQ-1 ( JQ1)

(S)-(+)-Tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]