WZ4003 - CAS:1214265-58-3 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	WZ4003
英文名称:	WZ4003
别名:	N-[3-[[5-chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-propanamide
CAS No:	1214265-58-3	分子式:	C₂₅H₂₉ClN₆O₃	分子量:	496.1
CAS No:	1214265-58-3
分子式:	C₂₅H₂₉ClN₆O₃
分子量:	496.1
MDL:	MFCD28015100

安全技术说明书(PDF) MSDS(PDF) 点击下载技术规格说明书(PDF) 点击下载产品说明书(PDF)

W10003 WZ4003 ≥98%(HPLC) (psaitong)

相关产品

包装规格：

25mg 100mg in glass bottle

溶解性：

溶于DMSO(7mg/mL)

产品描述：

基本信息

产品编号：W10003
产品名称：WZ4003
CAS:	1214265-58-3	储存条件	粉末	-20℃	四年

分子式：	C25H29ClN6O3		溶于液体	-80℃	六个月
分子量：	496.10			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	7mg/mL (14.08mM)
		Ethanol	Insoluble
		Water	Insoluble
	体内（现配现用）
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.0121mL	10.0606mL	20.1211mL
5mM	0.4024mL	2.0121mL	4.0242mL
10mM	0.2012mL	1.0061mL	2.0121mL

生物活性

产品描述	一种选择性的LKB1肿瘤抑制因子激活的NuAK激酶抑制剂,抑制NuAK异构体,NuAK1的IC50为20nm，NuAK2为100nm。
靶点/IC50	NUAK1 (Cell-free assay)	NUAK2 (Cell-free assay)
	20nM	100nM
体外研究	WZ4003 (3-10μM) markedly suppresses NUAK1-mediated MYPT1 phosphorylation,in HEK-293 cells expressing wild-type NUAK1.Moreover,WZ4003 (10μM) inhibits MYPT1 Ser445 phosphorylation as well as cell migration,invasion and proliferation to a similar extent as knock out in MEFs or knock down in U2OS cells of NUAK1.WZ4003 also exhibits a high,specific affinity to the L858R/T790M mutant EGFR,while a significantly reduced cellular IC50 against T790M containing Ba/F3 cells.

推荐实验方法(仅供参考)

激酶实验：

In vitro activities of purified GST-NUAK1 and GST-NUAK1[A195T] are measured using Cerenkov counting of incorporation of radioactive 32P from [γ-32P]ATP into Sakamototide substrate peptide.Reactions are carried out in a 50μL reaction volume for 30 min at 30℃and reactions are terminated by spotting 40μL of the reaction mix on to P81 paper and immediately immersing in 50mM orthophosphoric acid.Samples are washed three times in 50mM orthophosphoric acid followed by a single acetone rinse and air drying.The kinase-mediated incorporation of [γ-32P]ATP into Sakamototide is quantified by Cerenkov counting. One unit of activity is defined as that which catalysed the incorporation of 1nmol of [32P]phosphate into the substrate over 1h.MCE has not independent

细胞实验:
Cell proliferation assays are carried out colorimetrically in 96-well plates.Initially,2000 cells per well are seeded for U2OS cells and 3000 cells per well are seeded for MEFs.The proliferation assays are carried out over 5 days in the presence or absence of 10μM HTH-01-015 or WZ4003.