Encorafenib-LGX818-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEncorafenibCat. No.: HY-15605CAS No.: 1269440-17-6Synonyms: LGX818分式: CHClFNOS分量: 540.01作靶点: Raf作通路: MAPK/ERK Pathway储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (92.59 mM; Need

2、 ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.8518 mL 9.2591 mL 18.5182 mL5 mM 0.3704 mL 1.8518 mL 3.7036 mL10 mM 0.1852 mL 0.9259 mL 1.8518 mL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，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件

3、，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.63 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.63 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您边的

4、抑制剂师www.MedChemESolubility: 2.5 mg/mL (4.63 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Encorafenib (LGX818)种效的 BRAF 抑制剂，对BRAFV600E 细胞有选择性抗增殖和促凋亡活性，EC50值为4 nM。IC50 & Target IC50: 0.3 nM (BRafV600E)体外研究 Encorafenib (LGX818) is a potent drug that can prevents diseases or disorders associated with abnorm

5、al orderegulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf 1.Encorafenib (LGX818) (10 nM) suppresses the ERK/MAPK pathway and displays marked inhibition of pERKin A375, G361 and SK-MEL-24 cells. 10 nM Encorafenib (LGX818) treatment for 12 days pote

6、ntly inhibitscolony formation in A375, G361 and SK-MEL-24 cells, but not in RPMI7951 and C8161 cells. Encorafenib(LGX818) treatment induces a steady increase in the -catenin level in G361 cells over time 2.户使本产品发表的科研献 Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. Sci Adv. 2019 Aug.See more cus

7、tomer validations on HYPERLINK / www.MedChemEREFERENCES1. Compounds and compositions as protein kinase inhibitors. Patent WO 2011025927 A12. Li Z, et al. Encorafenib (LGX818), a potent BRAF inhibitor, induces senescence accompanied by autophagy in BRAFV600E melanomacells. Cancer Lett. 2016 Jan 28;370(2):332-44.McePdfHeightCaution: Product has not been fully validated for medical applications.For research