JQEZ5 - Histone Methyltransferase 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEJQEZ5Cat. No.: HY-100846CAS No.: 1913252-04-6分式: CHNO分量: 542.68作靶點(diǎn): Histone Methyltransferase作通路: Epigenetics儲(chǔ)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(shí)驗(yàn) DMSO : 25 mg/mL (46.07 mM; Need ultraso

2、nic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.61 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 JQEZ5種新型強(qiáng)效 EZH2 抑制劑。IC50 & Target EZH2 1體內(nèi)研究 Animals treated with JQEZ5 exhibit rapid and pronounced tumor regression over the three week

3、treatmentcourse. H3K27me3 levels are largely reduced with treatment further confirming the on-target effect of JQEZ5in mice. The level of H3K27me3 is largely reduced with the treatment without effect on EZH2 levels in both thetumor and in the lung tissue of JQEZ5 treated animals 1.PROTOCOLAnimal Tum

4、or-bearing genetically-engineered mouse models (GEMMs) are monitored for onset of symptoms (breathAdministration 1 distress) and then treated with JQEZ5 for three weeks (75 mg/kg IP daily). Tumors are visualized by MRI andtumor volume of the lungs is calculated using 3D Slicer. For xenograft experim

5、ents, H661 cells aredissociated into single cells, counted and resuspended at 2106 cells per 250 L of 1:1 media/matrigel.Eight- to 12-week-old female Foxn1nu/Foxn1nu mice are injected subcutaneously with 2106 cells in two tothree spots on the flanks. Tumors are allowed to grow to an approximate size

6、 of 200 mm3 (10 weeks) andthe mice are randomized for vehicle (n=3) or JQEZ5 administration (n=6, 75 mg/kg/d, i.p.) for 18 days. Tumorgrowth is measured by caliper measurements and tumor volume is calculated by standard methods 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Zhang H, et al. Oncogenic Deregulation of EZH2 as an Opportunity for Targeted Therapy in Lung Cancer. Cancer Discov. 2016Sep;6(9):1006-21.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use onl