产品说明书

G007-LK

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Chemical Structure| 1380672-07-0 同义名 : Tankyrase 1/2 Inhibitor VI
CAS号 : 1380672-07-0
货号 : A341670
分子式 : C25H16ClN7O3S
纯度 : 99%+
分子量 : 529.958
MDL号 : MFCD28167833
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(56.61 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 G007-LK effectively inhibits TNKS1 and TNKS2, with IC50 values of 46 nM and 25 nM, respectively, and demonstrates a cellular IC50 of 50 nM. It does not inhibit PARP1 at concentrations up to 20 μM and possesses a high IC50 value for CYP3A4 inhibition (>25 μM)[1]. G007-LK (0-20 μM) inhibits the growth of hepatocellular carcinoma (HCC) cells in a dose-dependent manner. It reduces YAP levels by increasing AMOTL1 and AMOTL2 in HCC cell lines. Moreover, G007-LK (0-20 μM) works in synergy with MEK and AKT inhibitors to curb HCC cell proliferation[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.89mL

0.38mL

0.19mL

9.43mL

1.89mL

0.94mL

18.87mL

3.77mL

1.89mL
参考文献

[1]Voronkov A, 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]Norum JH, et al. The tankyrase inhibitor G007-LK inhibits small intestine LGR5+ stem cell proliferation without altering tissue morphology. Biol Res. 2018 Jan 9;51(1):3.

[3]Xin Chen, et al. Tankyrase inhibitors suppress hepatocellular carcinoma cell growth via modulating the Hippo cascade. PLoS One. 2017 Sep 6;12(9):e0184068.