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G007-LK  ≥98%

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包装规格：5mg 10mg 25mg 100mg in glass bottle
溶解性：溶于DMSO（≥30mg/mL）
产品描述：基本信息 产品编号：G10431 产品名称：G007-LK CAS: 1380672-07-0   储存条件 粉末 -20℃ 四年     分子式： C25H16ClN7O3S 溶于液体 -80℃ 两年 分子量 529.96 -20℃ 一个月 化学名：  4-{5-[(E)-2-{4-(2-Chlorophenyl)-5-[5-(Methylsulfonyl)pyridin-2-Yl]-4h-1,2,4-Triazol-3-Yl}ethenyl]-1,3,4-Oxadiazol-2-Yl}benzonitrile   Solubility (25°C)   体外 DMSO 100mg/mL (188.69mM) Ethanol Insoluble Water Insoluble 体内 现配现用   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 1.8869mL 9.4347mL 18.8693mL 5mM 0.3774mL 1.8869mL 3.7739mL 10mM 0.1887mL 0.9435mL 1.8869mL 50mM 0.0377mL 0.1887mL 0.3774mL   生物活性 产品描述 一种有效的，选择性的 TNKS1 和 TNKS2 抑制剂，IC50值分别为 46nM 和 25nM。 靶点/IC50 TNKS2 (Cell-free assay) 25nM TNKS1 (Cell-free assay) 46nM 体外研究 G007-LK is a potent inhibitor of TNKS1 and TNKS2, with IC50s of 46nM and 25nM, respectively, and a cellular IC50 of 50nM. G007-LK shows no inhibition of PARP1 at doses up to 20μM, and has a high CYP3A4 inhibition IC50 value (>25μM). G007-LK (0-20μM) 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 (0-20μM) 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 (100mg/kg chow, p.o.) significantly reduces lineage tracing from LGR5+ intestinal stem cells in mice. G007-LK (100mg/kg chow, p.o.) specifically targets LGR5+ WNT-dependent intestinal stem cells in Lgr5-EGFP-CreERT2;R26R-tdTomato mice. G007-LK (10, 50mg/kg, p.o.) also suppressses canonical WNT signalling. Furthermore, G007-LK (100, 1000mg/kg chow, p.o) shows no effect on the alteration of duodenal morphology .   推荐实验方法(仅供参考) 细胞实验： Cell Assay For cell proliferation or apoptosis assays, SNU-449 and HLE cells are grown in a 5% CO2 atmosphere, at 37°C, in RPMI Medium supplemented with 10% fetal bovine serum (FBS) and penicillin/streptomycin. HCC cells are treated with 0.1% DMSO, or 2.5μM, 5μM, 10μM, 20μM XAV-939 or G007-LK, either alone or in combination with the MEK inhibitor U0126 (25μ M) or the AKT inhibitor MK-2206 (5μM). Cell proliferation is analyzed using the BrdU Cell Proliferation Assay Kit, while apoptosis is assessed with the Cell Death Detection Elisa Plus Kit.   动物实验:   Animal Administration Drug treatment experiments are performed with wild type (wt), single or double transgenic Lgr5-EGFP-Ires-CreERT2;R26RConfetti mice, unless indicated otherwise. G007-LK is administered orally either by gavage (10 or 50mg/kg body mass once daily, vehicle: 15% dimethylsulfoxide [DMSO], 17.5% Cremophor EL, 8.75% Miglyol 810 N, 8.75% ethanol in phosphate buffered saline [PBS]) or in G007-LK enriched chow (100 or 1000mg G007-LK/kg chow ad libitum, corresponding to a daily G007-LK dose of approximately 20 or 200mg/kg body mass, respectively, for a mouse with a body mass of 25 g and consumption of approximately 5g enriched diet/day). G007-LK treatments are initiated at the age of 5 weeks and 5 days for oral gavage treatment or 6 weeks for enriched chow administration and continued for 9 or 21 days, respectively .
保存条件：-20℃

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