XMD8-87-ACK1-B19-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEXMD8-87Cat. No.: HY-15811CAS No.: 1234480-46-6Synonyms: ACK1-B19分式: CHNO分量: 445.52作靶点: Tyrosinase作通路: Metabolic Enzyme/Protease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 : 26 mg/mL (58.3

2、6 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.67 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.08 mg/mL (4.67 mM); Suspended solution; Need ultrasonicBIOLOGICAL ACTIVITY物活性 XMD8-87种有效的TNK2抑制剂

3、，对于D163E和R806Q突变体的IC50值分别为38和113 nM。IC50 & Target IC50: 38 nM (TNK2, D163E mutation), 113 nM (TNK2, R806Q mutation) 1体外研究 XMD8-87 potently inhibits the growth of the TNK2 mutant expressing cell lines while having little or no effecton the control cells out to the highest tested concentrations (1,000

4、 nM). XMD8-87 has IC50s of 38 nM and113 nM for the D163E and R806Q mutations. The effects of XMD8-87 on TNK2 cell lines are largely due toon-target effects on TNK2. Auto-phosphorylation of overexpressed TNK2 mutants could be blocked withTNK2 inhibitor XMD8-87 1.PROTOCOLKinase Assay 1 Kinase targets

5、are tested with biochemical enzymatic kinase assays using the SelectScreen Kinase ProfilingService to determine IC50 values. The compounds (XMD8-87) are assayed at 10 concentrations (3-foldserial dilutions starting from 1 M) at an ATP concentration equal to the ATP Km 1.MCE has not independently con

6、firmed the accuracy of these methods. They are for reference only.Cell Assay 1 Cells are treated with the following inhibitors for 72 hours: dasatinib, AIM-100, XMD8-87 and XMD16-5. Cellviability is measured using a methanethiosulfonate (MTS)-based assay and absorbance (490 nm) is read at 1and 3 hou

7、rs after adding reagent 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Maxson JE, et al. Identification and Characterization of Tyrosine Kinase Nonreceptor 2 Mutations in Leukemia through Integration ofKinase Inhibitor Screening and Genomic Analysis.McePdfHeightCaution: Product has not been fully validated for medical applications.For research