规格

价格

库存

数量

1 mg

¥ 397

现货

2 mg

¥ 593

现货

5 mg

¥ 987

现货

10 mg

¥ 1,570

现货

25 mg

¥ 2,830

现货

50 mg

¥ 4,180

现货

100 mg

¥ 5,990

现货

1 mL x 10 mM (in DMSO)

¥ 1,160

现货

生物活性

产品描述	G007-LK is a selective inhibitor of TNKS1 and TNKS2, with IC50s of 46 nM and 25 nM, respectively.
靶点活性	TNKS1:46 nM, TNKS2:25 nM
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。
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.
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.
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

化学信息

分子量	529.96
分子式	C₂₅H₁₆ClN₇O₃S
CAS No.	1380672-07-0
Smiles	CS(=O)(=O)c1ccc(nc1)-c1nnc(\C=C\c2nnc(o2)-c2ccc(cc2)C#N)n1-c1ccccc1Cl
密度	1.47 g/cm3 (Predicted)
颜色	White
物理性状	Solid

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 93 mg/mL (175.48 mM), Sonication is recommended.

体内实验配方

10% DMSO+90% Corn Oil: 3.3 mg/mL (6.23 mM), Sonication is recommeded.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8869 mL	9.4347 mL	18.8693 mL	94.3467 mL
5 mM	0.3774 mL	1.8869 mL	3.7739 mL	18.8693 mL
10 mM	0.1887 mL	0.9435 mL	1.8869 mL	9.4347 mL
20 mM	0.0943 mL	0.4717 mL	0.9435 mL	4.7173 mL
50 mM	0.0377 mL	0.1887 mL	0.3774 mL	1.8869 mL
100 mM	0.0189 mL	0.0943 mL	0.1887 mL	0.9435 mL