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CAS No.: 1380672-07-0

G007-LK Catalog No. CSN17770

Synonyms: Tankyrase 1/2 Inhibitor VI

G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述G007-LK is a high selective inhibitor of both tankyrases 1 and 2 with IC50 values of 46 nM and 25 nM, respectively. Treatment with G007-LK at concentration>1μM reduced Wnt/β-catenin signaling by preventing poly(ADP-ribosyl)ation-dependent AXIN degradation, thereby promoting β-catenin destabilization in SW480 cells and COLO-320DM cells. G007-LK at concentration of 0.2μM inhibited colony formation of COLO-320DM and SW403 cells post 7-day treatment. Also inhibition of cell-cycle progression and induction of differentiation could be observed post G007-LK treatment. Intraperitoneal injection with G007-LK at dose of 20, 40 and 60mg/kg, QD, or at dose of 10, 20 and 30mg/kg, BID, for 21 days could dose-dependently inhibited tumor growth in COLO-320DM xenograft mice, with obvious body weight loss only at dose of 30 and 60mg/kg post 16-day treatment. Administration of 100mg/kg G007-LK through chow for 3 weeks inhibited WNT signalling in LGR5⁺ stem cells and reduced the number and distribution of cells traced from duodenal LGR5⁺ stem cells of Lgr5-EGFP-Ires-CreERT2;R26R-Confetti mice.
动物研究
剂量
Mice: 0 mg/kg - 100 mg/kg^[2] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 0 mg/kg - 100 mg/kg^[2] (i.p.)
给药途径	i.p.

[1] Voronkov A, Holsworth DD, et al. Structural basis and SAR for G007-LK, a lead stage 1,2,4-triazole based specific tankyrase 1/2 inhibitor. J Med Chem. 2013 Apr 11;56(7):3012-23.
[2] Lau T, Chan E, et al. A novel tankyrase small-molecule inhibitor suppresses APC mutation-driven colorectal tumor growth. Cancer Res. 2013 May 15;73(10):3132-44.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8869 mL
- 9.4347 mL
- 18.8694 mL
- 5 mM
- 0.3774 mL
- 1.8869 mL
- 3.7739 mL
- 10 mM
- 0.1887 mL
- 0.9435 mL
- 1.8869 mL

技术信息

CAS号

1380672-07-0

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H16ClN7O3S

运输

蓝冰

分子量

529.96

别名

Tankyrase 1/2 Inhibitor VI

溶解度

DMSO	35.0 mg/mL (66.0 mM)
Water	insoluble

动物实验配方

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