WZ-3146 _EGFR 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEWZ-3146Cat. No.: HY-12001CAS No.: 1214265-56-1分式: CHClNO分量: 464.95作靶点: EGFR作通路: JAK/STAT Signaling; Protein Tyrosine Kinase/RTK储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 150 mg/mL (322

2、.62 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.1508 mL 10.7538 mL 21.5077 mL5 mM 0.4302 mL 2.1508 mL 4.3015 mL10 mM 0.2151 mL 1.0754 mL 2.1508 mL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，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；

3、澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.38 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.38 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/

4、mL (5.38 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 WZ3146是突变选择性的 EGFR 抑制剂；对EGFRL858R，EGFRL858R/T790M，EGFRE746_A750，EGFRE746_A750/T790M and EGFR 的 IC50 值分别为2，2，5，14 和 66 nM。IC50 & Target EGFRL858R EGFRL858R/T790M EGFRE746_A750 EGFRE746_A750/T790M2 nM (

5、IC50) 5 nM (IC50) 2 nM (IC50) 14 nM (IC50)EGFR24 nM (IC50)体外研究 WZ3146 is a novel EGFR inhibitor, suppresses the growth of EGFR T790M containing cell lines and inhibitsEGFR phosphorylation 1.PROTOCOLKinase Assay 1 In vitro inhibitory enzyme kinetic assays are carried out in triplicate using the ATP/N

6、ADH coupled assaysystem in a 96-well format. The final reaction mixture contains 0.5mg/mL Bovine Serum Albumin (BSA), 2mMMnCl2, 1mM phospho(enol) pyruvic acid, 1mM TCEP, 0.1M Hepes 7.4, 2.5mM poly-Glu4Tyr1 peptide, 1/50of the final reaction mixture volume of pyruvate kinase/lactic dehydrogenase enzy

7、mes from rabbit muscle,0.5mM NADH, 0.5M EGFR kinase, 100M ATP and varied amount of inhibitors. Inhibitors and ATP aremixed and made separate stock from the mixture with all other ingredients and added last to the latter to startthe reaction. Steady state initial velocity data are drawn from the slop

8、es of the A340 curves 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Growth and inhibition of growth is assessed by MTS assay. Ba/F3 cells are exposed to WZ3146 treatment forAdministration 1 72 hours. Growth and inhibition of growth is assesse

9、d by MTS assay 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Zhou W, et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.Nature. 2009 Dec 24;462(7276):1070-4.McePdfHeightCaution: Product has not been fully validated for medical