货号	规格	价格	上海	北京	珠海	重庆	武汉
Y47012-5mg买3赠1	99.20%	￥520.00 Y47012-5mg ￥520.00 现货（买3赠1）	5 5	-	-	-	-
Y47012-10mg买3赠1	99.20%	￥800.00 Y47012-10mg ￥800.00 现货（买3赠1）	6 6	-	-	-	-
Y47012-25mg促销	99.20%	￥1600.00 ￥1280.00 Y47012-25mg ￥1280.00 现货	1 1	-	-	-	-
Y47012-100mg促销	≥98%	￥4130.00 ￥3300.00 Y47012-100mg ￥3300.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

UNC0642 is an effective and specific G9a/GLP inhibitor (IC50< 2.5 nM).

靶点：

GLP:<2.5 nM, G9a:<2.5 nM;HistoneMethyltransferase

体外研究：

UNC0642 (Ki: 3.7±1 nM) is competitive with the peptide substrate and non-competitive with the cofactor SAM. UNC0642 is more than 300-fold selective for G9a and GLP over a broad range of kinases, transporters, GPCRs, and ion channels. UNC0642 exhibits high potency at low cell toxicity, reducing the H3K9me2 mark, and good separation of functional potency in a number of cell lines

体内研究：

UNC0642 (5 mg/kg, i.p.) results in a plasma Cmax of 947 ng/mL and an AUC of 1265 h·ng/ml.

细胞实验：

MDA-MB-231, PC3, and U2OS cells are treated with UNC0642 for 48 h. Cell viability assays are performed by incubating cells with 0.1 mg/mL of resazurin for 3 – 4 h. Resazurin reduction is monitored with 544 nm excitation, measuring fluorescence at 590 nm

动物实验：

Mouse: Standard PK studies are performed using male Swiss albino mice. Plasma and brain concentrations are measured at 0.08, 0.25, 0.5, 1, 2, 4, 8, and 24 h following UNC0642 (5 mg/kg, i.p.). The compound concentration at each time point in plasma or brain is the average value from 3 test animals

参考文献：

1. Liu F, et al. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J Med Chem. 2013 Nov 14;56(21):8931-42. doi: 10.1021/jm401480r. Epub 2013 Oct 31.

溶解性：

Soluble in DMSO

保存条件：

2-8°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.829 ml	9.146 ml	18.292 ml
5 mM	0.366 ml	1.829 ml	3.658 ml
10 mM	0.183 ml	0.915 ml	1.829 ml
50 mM	0.037 ml	0.183 ml	0.366 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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UNC0642

2-(4,4-Difluoro-1-piperidinyl)-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)