货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T96260-1ml促销	10mM in DMSO	￥720.00 ￥648.00 T96260-1ml ￥648.00 现货	4 4	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T96260-1ml促销

10mM in DMSO

￥720.00 ￥648.00

产品描述：

c-RET 抑制剂;c-RET Inhibitors;;InformationGSK3179106 GSK3179106 is a potent, selective, and gut-restricted pyridone hinge binder small molecule RET (c-RET) kinase inhibitor with a RET IC50 of 0.3 nM and is efficacious in vivo.TargetsRET (Cell-free assay) 0.3 nMIn vitroGSK3179106 has a clean genotoxic profile with no embedded genotoxicity liabilities and possesses good kinase selectivity: only 26 out of a set of >300 recombinant kinases are found to be inhibited at a 1 μM test concentration.In vivoSingle dose IV (bolus, 0.06 mg/kg) PK in male Sprague-Dawley rats of compound GSK3179106 formulated as 0.04 mg/mL in DMSO/6% HP-beta-CD = 5:95 with a pH of 7 as a clear solution shows low exposure with an AUC of 102 ng·h/mL. Oral PK is evaluated with the same dosing regimen as the in vivo colonic hypersensitivity model, seven doses of 10 mg/kg given over 3.5 days. Full gut PK measurements are also taken to help understand the PK/PD relationship--It reveals high concentrations of GSK3179106 in the colon contents, jejunum, duodenum, and ileum, over that in plasma.

靶点：

IC50: 0.4 nM (human RET), 0.2 nM (rat RET)

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.139 ml	10.697 ml	21.394 ml
5 mM	0.428 ml	2.139 ml	4.279 ml
10 mM	0.214 ml	1.07 ml	2.139 ml
50 mM	0.043 ml	0.214 ml	0.428 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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