KO-947 - ERK 抑制劑 - 生命科學試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEKO-947Cat. No.: HY-112181CAS No.: 1695533-89-1分式: CHNO分量: 355.39作靶點: ERK作通路: MAPK/ERK Pathway; Stem Cell/Wnt儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 62.5 mg/mL (175.86 mM; Need ultra

2、sonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.8138 mL 14.0691 mL 28.1381 mL5 mM 0.5628 mL 2.8138 mL 5.6276 mL10 mM 0.2814 mL 1.4069 mL 2.8138 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)實驗 請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保

3、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: 2.08 mg/mL (5.85 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.85 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.85 mM); C

4、lear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 KO-947有效和選擇性的 ERK1/2 激酶抑制劑，在MAPK途徑失調(diào)的腫瘤中具有潛在的臨床效。IC50 & Target ERK1 ERK2體外研究 KO-947 is a 10 nM inhibitor of ERK with at least 50-fold selectivity against a panel of 450 kinases. KO-947blocks ERK signaling and prolif

5、eration of tumor cells exhibiting dysregulation of MAPK pathway signaling,including mutations in BRAF, NRAS or KRAS, at low nanomolar concentrations 1.體內(nèi)研究 In cell-line derived xenograft studies, KO-947 profoundly suppresses ERK signaling for up to five days after asingle dose and induces regression

6、s in RAS- and RAF-mutant melanoma, NSCLC and pancreatic cancermodels on administration schedules ranging from daily to weekly. Intermittent dosing enables comparableantitumor activity at reduced dose-intensity 1.REFERENCES1. Burrows F, et al. KO-947, a potent ERK inhibitor with robust preclinical si

7、ngle agent activity in MAPK pathway dysregulated tumorsabstract. In: Proceedings of the American Association for Cancer Research Annual Meeting 2017; 2017 Apr 1-5; Washington, DC.Philadelphia (PA): AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 5168. doi:10.1158/1538-7445.AM2017-5168.McePdfHeightCaution: Product has not been fully validated for medical applications.For research us