化合物EPZ020411 HCl T22325

Product Introduction
Bioactivity


英文名: EPZ020411 hydrochloride

描述: EPZ020411 hydrochloride 是一种选择性的和有效的 PRMT6抑制剂，IC50=10 nM。

细胞实验: Cell lines: A375 cells. Concentrations: 0-20 μM. Incubation Time: 48 h. Method: A375 (CRL-1619) cells are cultured in DMEM with 10% (vol/vol) FBS. PRMT6 is cloned into EcoRI and BamHI sites of a pcDNA4 HisMAX_A plasmid. According to procedures recommended by the manufacturer, transfection of his-tagged PRMT6 or vector control is carried out using Lipofectamine LTX and Plus reagent . Cells are seeded at 200,000 cells/well in 6-well plates. The second day, the cells are concurrently transfected and treated with compound in 0.25% DMSO. Cells are incubated in the presence compound at 20 μM and collected after 48 hours treatment.

动物实验: Animal Models: SD rats. Dosages: 1 mg/kg. Administration: i.v..

体外活性: Treatment with EPZ020411 results in a dose-dependent decrease in H3R2 methylation in A375 human melanoma cells exogenously overexpressing PRMT6(IC50=0.637±0.241 μM). EPZ020411 is over 100-fold selective for PRMT6/8/1 compared to other histone methyltransferases including PRMT3, PRMT4, PRMT5, and PRMT7 in biochemical assays. The compound shows poor permeability in the parallel artificial membrane permeation assay[1].

体内活性: EPZ020411 shows good bioavailability following subcutaneous dosing in rats. Male Sprague-Dawley rats administered EPZ020411 at a single dose of 1 mg/kg by i.v. bolus show a moderate clearance (CL) of 19.7±1.0 mL/min/kg, with a volume of distribution at steady state (Vss) of 11.1±1.6 L/kg, translating to a mean terminal half-life (t1/2) of 8.54±1.43 h. A good bioavailability of 65.6 ± 4.3% is observed following 5 mg/kg s.c. dosing, leading to EPZ020411 unbound blood concentration remaining above the PRMT6 biochemical IC50 for more than 12 h[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 18.0 mg/mL (37.6 mM)
DMSO : 45.0 mg/mL (93.9 mM)


关键字: EPZ 020411 Hydrochloride | EPZ-020411 hydrochloride | EPZ020411 Hydrochloride | EPZ-020411 Hydrochloride | EPZ020411 hydrochloride

相关产品: BCI-121 | Tazemetostat | OICR-9429 | Valemetostat | PF-06726304 | JQEZ5 | AMI-1 | EZH2-IN-15 | BIX-01294 | MRTX9768

相关库: Bioactive Compounds Library Max | Inhibitor Library | Epigenetics Compound Library | Covalent Inhibitor Library | Histone Modification Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途