G007-LK
| 中文名称 | G007-LK |
|---|---|
| 中文同义词 | 4-[5-[(1E)-2-[4-(2-氯苯基)-5-[5-(甲基磺酰基)-2-吡啶基]-4H-1,2,4-三唑-3-基]乙烯基]-1,3,4-恶二唑-2-基]苯甲腈;TANKYRASE抑制剂(G007-LK);G007-LK游离态;G007-LK游离;化合物G007-LK;(E)-4-(5-(2-(4-(2-氯苯基)-5-(5-(甲磺酰基)吡啶-2-基)-4H-1,2,4-三唑-3-基)乙烯基)-1,3,4-恶二唑-2-基)苯甲腈 |
| 英文名称 | G007-LK |
| 英文同义词 | G007-LK;(E)-4-(5-(2-(4-(2-chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)vinyl)-1,3,4-oxadiazol-2-yl)benzonitrile;4-[5-[(1E)-2-[4-(2-Chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]benzonitrile;Benzonitrile, 4-[5-[(1E)-2-[4-(2-chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]-;G007-LK;G007 LK;G007LK;CS-1659;Tankyrase 1/2 Inhibitor VI, G007-LK - Calbiochem;G007 LK;G007LK |
| CAS号 | 1380672-07-0 |
| 分子式 | C25H16ClN7O3S |
| 分子量 | 529.96 |
| EINECS号 | |
| 相关类别 | 细胞生物学试剂 |
| Mol文件 | 1380672-07-0.mol |
| 结构式 |  |
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 |
| 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.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-12438 | G007-LK G007-LK | 1380672-07-0 | 2mg | 800元 |
| 2024/04/30 | S7239 | G007-LK G007-LK | 1380672-07-0 | 5mg | 1188.88元 |