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• 产品描述： G007-LK是一种有效的选择性tankyrase抑制剂，对TNKS1/2的IC50分别为46 nM 和 25 nM

• 靶点： TNKS2(Cell-free assay):25 nM; TNKS1(Cell-free assay):46 nM;PARP;Wnt/beta-catenin

• 体外研究：
  G007-LK reduces Wnt/β-catenin signaling by preventing poly(ADP-ribosyl)ation-dependent AXIN degradation, thereby promoting β-catenin destabilization. G007-LK completely blocks ligand-driven Wnt/β-catenin signaling in cell culture and display approximately 50% inhibition of APC mutation–driven signaling in most CRC cell lines. G007-LK (0.2 μM) reduces the number of COLO-320DM cells in mitosis from 24% to 12% and decreases HCT-15 cells in S-phase from 28% to 18%. G007-LK suppresses colony formation in CRC lines COLO-320DM and SW403. G007-LK suppresses organoids growth with IC50 of 80 nM

• 体内研究：
  G007-LK exhibits antitumor efficacy in xenograft and genetically engineered CRC models. In the COLO-320DM model, G007-LK reduces tankyrases 1 and tankyrases 2 protein levels, stabilizes AXIN1 and AXIN2, and decreases β-catenin level. Wnt/β-catenin signaling is clearly inhibited in a dose-dependent manner in the efficacy study tumors as indicated by reduced expression of β-catenin–activated genes NKD1, APCDD1, and TNFRSF19 (TROY), as well as increased expression of β-catenin–repressed gene CLIC3. G007-LK treatment increases expression of KRT20 and TM4SF4 in COLO-320DM tumors. G007-LK (20 mg/kg twice daily) achieves 61% tumor growth inhibition. G007-LK reduces Wnt/β-catenin signaling and cell proliferation in normal intestine

• 细胞实验： Cell lines: APC-mutant CRC cell lines COLO-320DM Concentrations: ~0.2 μM Incubation Time: 7 to 13 days Method: For colony formation assays, cells are seeded at 500 cells/well in 2 mL of 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, changing medium and compound every third day. Colonies are stained by adding 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.

• 动物实验： Animal Models: Human APC –mutant CRC xenograft COLO-320DM Dosages: 20 mg/kg Administration: i.p. twice daily

• 参考文献：
  1. Voronkov A, et al. [1] Voronkov A, et al. J Med Chem, 2013, 56(7), 3012-3023. [2] Lau T, et al. Cancer Res, 2013, 73(10), 3132-3144.. J Med Chem, 2013, 56(7), 3012-3023. 2. Lau T, et al. A novel tankyrase small-molecule inhibitor suppresses APC mutation-driven colorectal tumor growth. Cancer Res, 2013, 73(10), 3132-3144.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.887 ml	9.435 ml	18.869 ml
  5 mM	0.377 ml	1.887 ml	3.774 ml
  10 mM	0.189 ml	0.943 ml	1.887 ml
  50 mM	0.038 ml	0.189 ml	0.377 ml

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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *