NSC139021-ERGi-USU-DataSheet-生命科學(xué)試劑-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作靶點: Others作通路: Others儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 62 mg/mL (242.85 mM)* means soluble,

2、but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的

3、儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (9.79 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (9.79 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性

4、 NSC139021 (ERGi-USU)ERG陽性癌細(xì)胞長的度選擇性抑制劑，抑制不同細(xì)胞系的 IC50 值為 30 到400nM。IC50 & Target IC50: 30 to 400 nM (ERG-positive cancer cells) 1體外研究 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.體內(nèi)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 您邊的抑制劑師www.MedChemEpii: canres.2949.2017.McePdfHeightCaution: Pro