(+)-JQ1

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(+)-JQ1

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	1268524-70-4
包装:	2mg, 5mg, 10mg, 50mg

包装与价格：

产品名称

JQ1

产品介绍

(+)-JQ1是一种BET bromodomain抑制剂，作用于BRD4(2)，IC50为33 nM，结合到BET家族的所有Bromodomain结构域，而不结合到BET家族以外的Bromodomain结构域，JQ1通过c-MYC介导的途径下调CD47的表达。

细胞实验
细胞系	MM.1S, RPMI-8226, KMS-20, L-363 Dox40 and AMO-1 cell lines
方法	Cell Viability Assays MM cell lines were seeded onto 384-well tissue culture treated plates at a density of 1,000 cells/well in a volume of 50 μL of media. After seeding cells were incubated for 1 hour and during the interim a stock plate of JQ1 was thawed at room temperature in a desiccated box. The addition of JQ1 to the assay plate was done with disposable 384-well pins (V&P Scientific, San Diego, CA) that delivered 100 nL of the drug diluted in DMSO to each well of the plate. After 72 hours of incubation cells were analyzed for cell viability by the addition of CellTiter Glo (Promega, Madison, WI) to the assay plates. After 30 min incubation at 37 oC the signal from the viable cells was analyzed on a Luminoskan luminometer (Labsystems Franklin, MA).
浓度	0~1μM
处理时间	72 h

动物实验
动物模型	SCID-beige mice orthotopically xenografted after intravenous injection with MM.1S-luc+ cells
配制	JQ1 in 10% cyclodextrine (Sigma)
剂量	50 mg/kg daily
给药处理	intra-peritoneally for 5 days/week, 2 weeks

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的K_m系数
	动物 A的K_m系数

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.1882 mL	10.9412 mL	21.8823 mL
5 mM	0.4376 mL	2.1882 mL	4.3765 mL
10 mM	0.2188 mL	1.0941 mL	2.1882 mL