化合物G007-LK T6842

Product Introduction
Bioactivity


英文名: G007-LK

描述: G007-LK 是 TNKS1 和 TNKS2 的选择性抑制剂，IC50 分别为 46 nM 和 25 nM。

细胞实验: Cell lines: APC-mutant CRC cell lines COLO-320DM. Concentrations: ~0.2 μM. Method: For colony formation assays,cells are seeded at 500 cells/well in 2 mL medium.Cell line in triplicate wells is treated with either 0.06% DMSO or compound in 0.06% DMSO and incubated for up to 17 days or until colonies became sufficiently large to quantify.Colonies are stained with 200 μL of 12 mM 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide to each well for 1 h,and colony numbers are quantitated with a GelCount scanner at 1200 dpi resolution.

激酶实验: TNKS1 and TNKS2 in vitro biochemical assays: G007-LK inhibitory activity at various doses (duplicates) is tested twice by TNKS1, TNSK2 Chemiluminescent Assay Kits, and the luminescence is measured.

动物实验: Animal Models: Human APC –mutant CRC xenograft COLO-320DM. Formulation: 15% DMSO,17.5% Cremophor EL,8.75% ethanol,8.75% Miglyol 810N,50% PBS. Dosages: 20 mg/kg. Administration: intraperitoneal injection twice daily

体外活性: G007-LK在异种移植和基因工程CRC模型中显示出抗肿瘤效力.在COLO-320DM模型中,G007-LK降低了tankyrases 1和tankyrases 2蛋白水平,稳定了AXIN1和AXIN2,并降低了β-catenin水平.G007-LK治疗增加COLO-320DM肿瘤中KRT20和TM4SF4的表达. G007-LK（20 mg/kg每日两次）达到61％的肿瘤生长抑制.G007-LK降低正常肠道中的Wnt/β-连环蛋白信号传导和细胞增殖.

体内活性: G007-LK通过防止多聚（ADP-核糖基）依赖性的AXIN降解来降低Wnt /β-连环蛋白信号传导,由此促进β-连环蛋白去稳定化。G007-LK在细胞培养中完全阻断配体驱动的Wnt/β-连环蛋白信号传导,并在大多数CRC细胞系中显示对约50％APC突变驱动的信号传导的抑制。 G007-LK（0.2 μM）将有丝分裂中的COLO-320DM细胞数量从24％降低至12％,并将S期中的HCT-15细胞从28％降低至18％。G007-LK抑制CRC系列COLO-320DM和SW403中的集落形成。 G007-LK抑制器官生长,IC50为80 nM。

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

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 93 mg/mL (175.5 mM)


关键字: G007LK | Inhibitor | poly ADP ribose polymerase | G-007-LK | G007 LK | PARP | inhibit | G007-LK

相关产品: AG14361 | Venadaparib | Boehmenan | Myristicin | Talazoparib tosylate | PARP-1-IN-3 | PJ34 | PI-1840 | 3-Aminobenzamide | PARP1-IN-8 

相关库: Wnt/Hedgehog/Notch Compound Library | Anti-Prostate Cancer Compound Library | Anti-Breast Cancer Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Colorectal Cancer Compound Library | Reprogramming Compound Library | Stem Cell Differentiation 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