货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
S84185-5mg	≥98%	￥1890.00 S84185-5mg ￥1890.00 3-5天	0 货期：3-5天	-	-	-	-
S84185-10mg	≥98%	￥2990.00 S84185-10mg ￥2990.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300

靶点：

IC50: 0.02 μM (CBP), 0.03 μM (EP300), 13 μM (BRD4);EpigeneticReaderDomain

体外研究：

GNE-272 is exquisitely selective for CBP/ EP300 and remarkably selective (650-fold) over BRD4. When tested at 10 μM in 35 kinase panel and 42 receptors off-target screening panel, GNE-272 does not inhibit any target at >30%. In addition, GNE-272 does not inhibit (>10 μM, top concentration) several cytochrome P450s (3A4, 1A2, 2C9, 2C19, 2D6). The compound has good potency in the BRET cellular assay. In an orthogonal measure of the target engagement, GNE-272 is shown to inhibit the expression of MYC10 (MV4−11 cell line) with an EC50 of 0.91 μM and good correlation between the BRET and MYC cellular assays is observed

体内研究：

GNE-272 demonstrates low clearance following a 1 mg/ kg intravenous dose in a mouse PK experiment and good oral bioavailability when dosed at 100 mg/kg, reaching an unbound Cmax of 26 μM. GNE-272 shows a marked antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.345 ml	11.724 ml	23.447 ml
5 mM	0.469 ml	2.345 ml	4.689 ml
10 mM	0.234 ml	1.172 ml	2.345 ml
50 mM	0.047 ml	0.234 ml	0.469 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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