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LCH-7749944

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Chemical Structure| 796888-12-5 同义名 : GNF-PF-2356
CAS号 : 796888-12-5
货号 : A1220481
分子式 : C20H22N4O2
纯度 : 99%+
分子量 : 350.414
MDL号 : MFCD04218695
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(713.44 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 P21-activated kinase 4 (PAK4), a serine/threonine protein kinase, has involved in the regulation of cytoskeletal reorganization, cell proliferation, gene transcription, oncogenic transformation and cell invasion. Moreover, PAK4 overexpression, genetic amplification and mutations were detected in a variety of human tumors, which make it potential therapeutic target. LCH-7749944 is a potent PAK4 inhibitor with an IC50 value of 14.93 μM. In MTT assay, LCH-7749944 treatment inhibited the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cells in a concentration dependent manner. Further, exposure of SGC7901 cells to various concentrations of LCH-7749944 for different hours (12 h, 24 h and 48 h) prominently induced a dose-dependent increase in the percentage of cells in G1 phase and decrease in S phase compared with the control group, indicating that LCH-7749944 can arrest SGC7901 cells in the G1-S phase of the cell cycle. Furthermore, exposure of SGC7901 to LCH-7749944 (5, 10, 20 and 30 μM) for 24 h dramatically decreased levels of phospho-PAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression in a dose-dependent manner. Moreover, In SGC7901 and BGC823 cell lines, a dose-dependent decrease in cell migration and invasiveness was seen following treatment with LCH-7749944. Notably, LCH-7749944 inhibited PAK4-induced filopodia in a dose-dependent manner. Removal of LCH-7749944 from the culture media restored the ability of cells filopodia formation indicating that the effect of LCH-7749944 is reversible in live cells[1].
作用机制 LCH 7749944 forms hydrogen bond with Leu398 of PAK4 binding site[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.85mL

0.57mL

0.29mL

14.27mL

2.85mL

1.43mL

28.54mL

5.71mL

2.85mL
参考文献

[1]Zhang J, Wang J, Guo Q, et al. LCH-7749944, a novel and potent p21-activated kinase 4 inhibitor, suppresses proliferation and invasion in human gastric cancer cells. Cancer Lett. 2012;317(1):24-32