1380672-07-0

中文名称 G007-LK

英文名称 G007-LK

CAS 1380672-07-0

分子式 C25H16ClN7O3S

分子量 529.96

MOL 文件 1380672-07-0.mol

更新日期 2024/04/29 17:03:09

1380672-07-0 结构式

基本信息物理化学性质安全数据图谱信息 G007-LK价格(试剂级) 常见问题列表

基本信息

中文别名

G007-LK游离态
TANKYRASE抑制剂(G007-LK)
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

英文别名

G007-LK
CS-1659
G007 LK
G007LK
G007-LK
G007 LK
G007LK
Tankyrase 1/2 Inhibitor VI, G007-LK - Calbiochem
(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]-

所属类别

生物化工：激动剂抑制剂

物理化学性质

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≥26.5 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH

酸度系数(pKa)-1.68±0.10(Predicted)

形态白色粉末

安全数据

危险性符号(GHS)

GHS06

警示词危险

危险性描述H301

防范说明P301+P310

图谱信息

G007-LK(1380672-07-0)核磁图(¹HNMR)

G007-LK价格(试剂级)

报价日期	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
2024/04/30	HY-12438	G007-LK G007-LK	1380672-07-0	5mg	1200元

常见问题列表

生物活性

G007-LK是一种有效的选择性tankyrase抑制剂，对TNKS1/2的IC50分别为46 nM 和 25 nM。

靶点

Target	Value
TNKS2 (Cell-free assay)	25 nM
TNKS1 (Cell-free assay)	46 nM

体外研究

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.

体内研究

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.