化合物PFI1 T6222

Product Introduction
Bioactivity


英文名: PFI-1

描述: PFI-1 (PF-6405761) 是一种BET 抑制剂，能有效抑制 BRD4，IC50值为 0.22 μM。

细胞实验: To determine dose response, cells are aliquoted into 96-well plate at 5 × 103 cells per well in triplicates. PFI-1 is added by 2- or 4-fold serial dilutions. Cell number is measured 5 days after plating using the CellTiter-Glo Kit and normalized to corresponding vehicle-treated groups. IC50 values are calculated by the GraphPad Prism 5 software using the 4-parameter logistic nonlinear regression model. To calculate the relative growth of cells, averaged cell titers of each group on day 1 are assigned a value of 1. All subsequent cell titer values are normalized accordingly. (Only for Reference)

体外活性: 在大鼠中,PFI-1 （1 mg/kg）静脉注射,分布体积为1 L/kg, 每分钟的血浆清除率为18mL/kg,半衰期为1小时.PFI-1（2 mg/kg）口服,有效性低至32%;PFI-1 (2 mg/kg)剂量皮下注射给药小鼠,Cmax 为58 ng/mL,Tmax 为1小时,半衰期约为2 小时.

体内活性: 在经脂多糖刺激的人血单核细胞中,PFI-1(EC50=1.89 μM) 抑制细胞产生的IL-6。在三种NET细胞系（胰腺NET衍生的Bon-1,和肺NET衍生的H727和H720）中,PFI-1抑制细胞增殖。在T4302 CD133+细胞中,PFI-1以剂量依赖的方式诱导细胞活力降低。PFI-1 （KD=49 μM）与cAMP反应结合元件结合蛋白结合。

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

溶解度: DMSO : 17.4 mg/mL (50 mM)


关键字: Inhibitor | PFI-1 | inhibit | PF 6405761 | Apoptosis | Autophagy | PF6405761 | Epigenetic Reader Domain

相关产品: Etalocib | physalin F | Genistein | AZ960 | INH1 | iCRT3 | Cholesteryl Hemisuccinate Tris Salt | Tasisulam | EC359 | JNJ-1013

相关库: Inhibitor Library | Kinase Inhibitor Library | Epigenetics Compound Library | Highly Selective Inhibitor Library | Apoptosis Compound Library | Autophagy Compound Library | Reprogramming Compound Library | Histone Modification Compound Library | NO PAINS 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