NSC139021-ERGi-USU-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENSC139021Cat. No.: HY-112158CAS No.: 1147-56-4Synonyms: ERGi-USU分式: CHNOS分量: 255.3作靶点: Others作通路: Others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 : 62 mg/mL (242.85 mM)* means soluble,

2、but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.9170 mL 19.5848 mL 39.1696 mL5 mM 0.7834 mL 3.9170 mL 7.8339 mL10 mM 0.3917 mL 1.9585 mL 3.9170 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；澄的

3、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 (9.79 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (9.79 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性

4、 NSC139021 (ERGi-USU)ERG阳性癌细胞长的度选择性抑制剂，抑制不同细胞系的 IC50 值为 30 到400nM。IC50 & Target IC50: 30 to 400 nM (ERG-positive cancer cells) 1体外研究 NSC139021 selectively inhibits growth of ERGpositive cancer cell lines with minimal effect on normalprostate or endothelial cells or ERG-negative tumor cell lines. The

5、 IC50 of NSC139021 for cell growthinhibition of responsive cell lines range between 30 nM to 400 nM. Combination of NSC139021 withenzalutamide shows additive effects in inhibiting growth of VCaP cells. A screen of kinases reveal thatNSC139021 directly bound the ribosomal biogenesis regulator atypica

6、l kinase RIOK2 and induces ribosomalstress signature 1.体内研究 NSC139021 treatment inhibits growth of ERG-positive VCaP tumor xenografts with no apparent toxicity.Significant (P 1.PROTOCOLCell Assay 1 To assess cell growth, To evaluate the ERG selectivity of the NSC139021, a panel of the following cell

7、 linesare assessed: ERG positive tumor cell lines (prostate cancer: VCaP; colon cancer: COLO320; leukemia: KG-1, MOLT-4; ERG negative prostate cancer cell lines (LNCaP, LAPC4, MDA PCa2b); normal prostateepithelium derived cell lines (BPH-1, RWPE-1); and primary endothelium derived cells (HUVEC). Mon

8、olayerof adherent cells are grown in their respective medium for 48 h followed by treatment with indicated dosageand time for the small molecule inhibitor NSC139021. Medium is replaced every 24 h containing the sameconcentration of the small molecule compound. Cells are counted by using trypan blue

9、exclusion method.Cell morphology is documented by photography in all indicated time points. IC50 is calculated usingGraphPad Prism 6 software 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 1Administration 1 The VCaP prostate cancer cells

10、are injected into lower right dorsal flank of the male athymic nude mice (6-8weeks old and weighing 27 to 30g). when tumors are palpable, mice are randomly separated into 2experimental groups and into one control group of 6 mice in each group. In the treatment groups mice areinjected intraperitoneal

11、ly (I.P) with 100 mg/kg of NSC139021 or 150 mg/kg of NSC139021 while the controlgroup are injected with vehicle (1:1v/v, DMSO/PEG300) only. Growth in tumor volume is recorded weeklyby using digital calipers and tumor volumes are calculated 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Mohamed AA, et al. Identification of a small molecule that selectively inhibits ERG-positive cancer cell growth. Cancer Res. 2018 Apr 30.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEpii: canres.2949.2017.McePdfHeightCaution: Pro