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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEML239Cat. No.: HY-19971CAS No.: 1378872-36-6分式: CHClNO分量: 346.6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 : 300 mg/mL (865.55 mM)* means soluble, but saturation unk

2、nown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.8852 mL 14.4259 mL 28.8517 mL5 mM 0.5770 mL 2.8852 mL 5.7703 mL10 mM 0.2885 mL 1.4426 mL 2.8852 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。BIOLOGICAL ACTIVITY物活性 ML239種有效的選擇性的乳腺癌腫瘤細胞抑制劑,C50 值為 1.16 M。體外研究ML239 (Compound 7j) is a potent and

3、 selective inhibitor of breast cancer stem cells, with an IC50 of 1.16 M,with -24-fold selectivity against the control cell line 1. ML239 inhibits breast cancer stem-like cells, mostlikely through activation of fatty acid desaturase 2 (FADS2). ML239 is cytotoxic to NCIH661 cells, and FADS2knockdown

4、reduces ML239 cytotoxicity, and furthermore, FADS2 inhibitor SC-26196 also reduces ML2391/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEcytotoxicity in cancer cell lines (CCLs) 2.PROTOCOLCell Assay 2 Cancer cell lines (CCLs) are plated at a density of 500 cells/well in white opaque tissue-culture-t

5、reatedAurora 1536-well MaKO plates in the provider-recommended growth media using a highly automatedplatform. Compounds (ML239) are added by acoustic transfer using a Labcyte Echo 555. 24 hours afterplating. The effects of small molecules (ML239) are measured over a 16-point concentration range (two

6、-folddilution) in duplicate. DMSO is used at a constant concentration of 0.33%, including vehicle-only controlwells. As a surrogate for viability, cellular ATP levels are assessed 72 hours after compound transfer byaddition of CellTiterGlo followed by luminescence measurement using a ViewLux Micropl

7、ate Imager.Duplicates are averaged and luminescence values normalized to vehicle (DMSO) treatment and background(media-only) wells 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Germain AR, et al. Identification of a selective small mole

8、cule inhibitor of breast cancer stem cells. Bioorg Med Chem Lett. 2012 May15;22(10):3571-4.2. Rees MG, et al. Correlating chemical sensitivity and basal gene expression reveals mechanism of action. Nat Chem Biol. 2016Feb;12(2):109-16.McePdfHeightCaution: Product has not been fully validated for medical applications.Fo

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