LCH-7749944

生物活性靶点体外研究 LCH-7749944 试剂级价格

LCH-7749944

CAS号:796888-12-5
英文名:LCH-7749944
中文名:LCH-7749944
CBNumber:CB42731092
分子式:C20H22N4O2
分子量:350.41
MOL File:796888-12-5.mol

LCH-7749944化学性质

沸点 :580.0±58.0 °C(Predicted)
密度 :1.272±0.06 g/cm3(Predicted)
储存条件 :2-8°C(protect from light)
溶解度 :DMSO: 250 mg/mL (713.45 mM)
酸度系数(pKa) :7.68±0.30(Predicted)
形态 :Solid
颜色 :White to off-white

LCH-7749944性质、用途与生产工艺

生物活性 LCH-7749944 (GNF-PF-2356) 是一种有效的 PAK4 抑制剂，IC50 为 14.93 μM。LCH-7749944通过下调 PAK4/c-Src/EGFR/cyclin D1 途径有效抑制人胃癌细胞的增殖，并诱导凋亡 (apoptosis)。
靶点

PAK4

14.93 μM (IC ₅₀ )

体外研究

LCH-7749944 (GNF-PF-2356; 5-50 μM; 24 hours) inhibits the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cells in a concentration dependent manner.
LCH-7749944 (5-20 μM; 12-48 hours) induces apoptosis of SGC7901 cells.
LCH-7749944 (5-20 μM; 12-48 hours) prominently induces a dose-dependent increase in the percentage of cells in G1 phase and decrease in S phase.
LCH-7749944 (5-30 μM; 24 hours) dramatically decreases levels of phosphoPAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression in a dose-dependent manner.

Cell Proliferation Assay

Cell Line:	MKN-1, BGC823, SGC7901 and MGC803 human gastric cancer cells
Concentration:	5, 10, 15, 20, 25, 30, 35, 40, 45, 50 μM
Incubation Time:	24 hours
Result:	Inhibited the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cells in a concentration dependent manner.

Apoptosis Analysis

Cell Line:	SGC7901 cells
Concentration:	5, 10, 20 μM
Incubation Time:	12, 24, 48 hours
Result:	Induced apoptosis of SGC7901 cells.

Cell Cycle Analysis

Cell Line:	SGC7901 cells
Concentration:	5, 10, 20 μM
Incubation Time:	12, 24, 48 hours
Result:	Prominently induced a dose-dependent increase in the percentage of cells in G1 phase and decrease in S phase.

Western Blot Analysis

Cell Line:	SGC7901 cells
Concentration:	5, 10, 20, 30 μM
Incubation Time:	24 hours
Result:	Dramatically decreased levels of phosphoPAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression in a dose-dependent manner.