化合物GDC-0084 T3705

Product Introduction
Bioactivity


英文名: GDC0084

描述: GDC0084 (RG7666) 是一种具有潜在抗肿瘤活性的 PI3K 抑制剂。 GDC0084 (RG7666) 特异性抑制 PI3K/AKT 激酶（或蛋白激酶 B）信号通路中的 PI3K，从而抑制 PI3K 信号通路的激活。这可能导致易感肿瘤细胞群中的细胞生长和存活受到抑制。

细胞实验: For transport studies, cells are seeded on 24-well Millicell plates 4 days prior to use(polyethylene terephtalate membrane, 1 μm pore size) at a seeding density of 1.3×105 cells/ml). GDC-0084 is tested at 5 μM in the apical-tobasolateral (A-B) and basolateral-to-apical (B-A) directions. The compound is dissolved in transport buffer consisting of Hanks' balanced salt solution with 10 mM HEPES. Lucifer Yellow is used as the paracellular and monolayer integrity marker. GDC-0084 concentrations in the donor and receiving compartments are determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis. The apparent permeability (Papp), in the apical to A-B and B-A directions, is calculated after 2-hour incubation.(Only for Reference)

体外活性: GDC-0084对小鼠脑中的PI3K信号通路有明显抑制效果,可抑制高达90%的pAkt信号.在U87和GS2原位移植瘤模型中,GDC-0084对肿瘤生长分别具有70%和40%的抑制作用.GDC-0084的疗效正处于临床患者检测评估阶段,暴露的耐受剂量与小鼠模型中的有效剂量一致.

体内活性: 在人微粒体及干细胞培养中,GDC-0084显示出良好的代谢稳定性,能抑制正常脑组织中PI3K通路的关键信号pAKT。GDC-0084抑制多种神经胶质瘤细胞的增殖（IC50：0.3-1.1 μM）。GDC-0084与血浆蛋白结合率较低,在CD-1小鼠血浆中游离分数为29.5±2.7%（n=3,5 μM）,而在CD-1小鼠中与脑组织结合率较高,游离分数只有6.7±1%(n=3)。

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

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 3.82 mg/mL (10 mM)


关键字: GDC0084 | RG-7666 | RG 7666

相关产品: Linperlisib | α-Solanine | Alpelisib | Erucic acid | PIK-90 | A66 | CH5132799 | LAS191954 | Autophinib | PI3K/HDAC-IN-1

相关库: Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Drug Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Diabetic Compound Library | Anti-Cancer Active Compound Library | Tyrosine Kinase Inhibitor Library | Stem Cell Differentiation 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