G007-LK
G007-LK 性质
| 沸点 | 817.3±75.0 °C(Predicted) |
|---|---|
| 密度 | 1.47±0.1 g/cm3(Predicted) |
| 储存条件 | +2C to +8C |
| 溶解度 | DMSO 中≥26.5 mg/mL；不溶于水；不溶于乙醇 |
| 形态 | 白色粉末 |
| 酸度系数(pKa) | -1.68±0.10(Predicted) |
| 颜色 | 米白色至黄色 |
G007-LK 用途与合成方法
| Target | Value |
|
TNKS2
(Cell-free assay) | 25 nM |
|
TNKS1
(Cell-free assay) | 46 nM |
G007-LK is a potent inhibitor of TNKS1 and TNKS2, with IC 50 s of 46 nM and 25 nM, respectively, and a cellular IC 50 of 50 nM. G007-LK shows no inhibition of PARP1 at doses up to 20 μM, and has a high CYP3A4 inhibition IC 50 value (>25 μM). G007-LK (0-20 μM) dose-dependently inhibits hepatocellular carcinoma (HCC) cell growth. G007-LK also downregulates the levels of YAP by upregulating AMOTL1 and AMOTL2 in HCC cell lines. In addition, G007-LK (0-20 μM) synergizes with MEK and AKT inhibitors to suppress HCC cell proliferation.
G007-LK displays great pharmacokinetic profile in ICR mice. G007-LK (100 mg/kg chow, p.o.) significantly reduces lineage tracing from LGR5 + intestinal stem cells in mice. G007-LK (100 mg/kg chow, p.o.) specifically targets LGR5 + WNT-dependent intestinal stem cells in Lgr5-EGFP-CreERT2;R26R-tdTomato mice. G007-LK (10, 50 mg/kg, p.o.) also suppressses canonical WNT signalling. Furthermore, G007-LK (100, 1000 mg/kg chow, p.o) shows no effect on the alteration of duodenal morphology.
G007-LK 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-11-08 | HY-12438 | G007-LK | 1380672-07-0 | 2mg | 800 |
| 2024-11-08 | S7239 | G007-LK | 1380672-07-0 | 5mg | 1188.88 |
