SW044248-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESW044248Cat. No.: HY-19637CAS No.: 522650-83-5分式: CHNOS分量: 421.52作靶点: Topoisomerase作通路: Cell Cycle/DNA Damage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 : 30 mg/mL (71.17 mM)* means solub

2、le, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3724 mL 11.8618 mL 23.7237 mL5 mM 0.4745 mL 2.3724 mL 4.7447 mL10 mM 0.2372 mL 1.1862 mL 2.3724 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。BIOLOGICAL ACTIVITY物活性 SW044248种典型的拓扑异构酶 I (topoisomerase I) 抑制剂，可以选择性地对某些细胞肺癌

3、细胞产毒性。IC50 & Target Topoisomerase I体外研究SW044248 is a non-canonical Top1 inhibitor, and is selectively toxic for certain NSCLC cell lines. SW0442481/2 Master of Small Molecules 您边的抑制剂师www.MedChemEshows no effect on Top2. SW044248 (2, 5, 10 M) rapidly inhibits transcription, translation and DNAsynthes

4、is in sensitive cells (HCC4017 and H292 cells) but not insensitive cells (HBEC30KT cells and HCC44cells). SW044248 (10 M) rapidly activates the integrated stress response through kinases GCN2 and PKR.The inhibition of Top1 in HCC4017 cells is helpful to the toxicity of SW044248. SW044248 (5, 10 M) s

5、howsno effect on HBEC30KT and HCC44 cell lines due to the up-regulation of p21CDKN1A 1. SW044248 isselectively toxic in 18/74 NSCLC lines 2.PROTOCOLCell Assay 1 100 L of 50,000 cells/mL cell suspensions of individual cell lines are added in wells in 96-well plates. Thenext day, 100 L of cell medium

6、substituted with 2X concentration of SW044248 or camptothecin or DMSO intriplicates is added to each well. After 96 and 120 hours the ATP concentration in the wells is measured withCelTiter-Glo. The luminescence is measured with an plate reader 1.MCE has not independently confirmed the accuracy of t

7、hese methods. They are for reference only.REFERENCES1. Zubovych IO, et al. A Novel Inhibitor of Topoisomerase I Is Selectively Toxic for a Subset of Non-Small Cell Lung Cancer Cell Lines. MolCancer Ther. 2016 Jan;15(1):23-36.2. Kim HS, et al. Systematic identification of molecular subtype-selective vulnerabilities in non-small-cell lung cancer. Cell. 2013 Oct24;155(3):552-66.McePdfHeightCaution: Product has not been fully validated for medical applications.For resear