1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELCH-7749944Cat. No.: HY-125035CAS No.: 796888-12-5分式: CHNO分量: 350.41作靶點(diǎn): PAK作通路: Cell Cycle/DNA Damage; Cytoskeleton儲存式: Please store the product under the recommended conditions inthe COA.溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 260 mg/mL (741.99 mM;

2、Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.8538 mL 14.2690 mL 28.5380 mL5 mM 0.5708 mL 2.8538 mL 5.7076 mL10 mM 0.2854 mL 1.4269 mL 2.8538 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄的儲備液，再依次添加助溶?為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲備液可以根據(jù)

3、儲存條件，適當(dāng)保存；以下溶劑前的百分指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.17 mg/mL (6.19 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.17 mg/mL (6.19 mM); Clear solutionBIOLOGICAL ACTIVITY物活性LCH-7749944種有效的 PAK4 抑制劑，IC50 為 14.93 M。L

4、CH-7749944通過下調(diào) PAK4/c-1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESrc/EGFR/cyclin D1 途徑有效抑制胃癌細(xì)胞的增殖，并誘導(dǎo)凋亡 (apoptosis)。IC50 & Target PAK414.93 M (IC50)體外研究LCH-7749944 (5-50 M; 24 hours) inhibits the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cellsin a concentration dependent manner 1.LCH-

5、7749944 (5-20 M; 12-48 hours) prominently induces a dose-dependent increase in the percentage ofcells in G1 phase and decrease in S phase 1.LCH-7749944 (5-30 M; 24 hours) dramatically decreases levels of phosphoPAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression in a dose-dependent ma

6、nner 1.LCH-7749944 (5-30 M; 24 hours) downregulates the mRNA level of cyclin D1 in SGC7901 1.LCH-7749944 (15 M) can induce apoptosis of SGC7901 cells 1.Cell Proliferation Assay 1Cell Line: MKN-1, BGC823, SGC7901 and MGC803 human gastric cancer cellsConcentration: 5, 10, 15, 20, 25, 30, 35, 40, 45, 5

7、0 MIncubation Time: 24 hoursResult: Inhibited the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cells in aconcentration dependent manner.Cell Cycle Analysis 1Cell Line: SGC7901 cellsConcentration: 5, 10, 20 MIncubation Time: 12, 24, 48 hoursResult: Prominently induced a dose-dependent increase

8、in the percentage of cells in G1 phaseand decrease in S phase.Western Blot Analysis 1Cell Line: SGC7901 cellsConcentration: 5, 10, 20, 30 MIncubation Time: 12, 24, 48 hoursResult: Dramatically decreased levels of phosphoPAK4, phospho-c-Src, phospho-EGFR andcyclin D1 protein expression in a dose-depe

9、ndent manner.RT-PCR 12/3 Master of Small Molecules 您邊的抑制劑師www.MedChemECell Line: SGC7901 cellsConcentration: 5, 10, 20, 30 MIncubation Time: 12, 24, 48 hoursResult: Downregulated the mRNA level of cyclin D1 in SGC7901.REFERENCES1. Zhang J, et al. LCH-7749944, a novel and potent p21-activated kinase 4 inhibitor, suppresses proliferation and invasion in human gastriccancer cells. Cancer Lett. 2012 Apr 1;317(1):24-32.McePdfHeightCaution: Product has not been fully validated for