1、Hotline: 400-820-3792 InhibitorsAgonistsScreening Libraries www.MedChemE PLX-4720 Cat. No.:HY-51424 CAS No.:918505-84-7 分式:CHClFNOS 分量:413.83 作靶点:Raf 作通路:MAPK/ERK Pathway 储存式:-20C3 yearsPowder 4C2 years -80C6 monthsIn solvent -20C1 month 溶解性数据 体外实验DMSO : 50 mg/mL (120.82 mM) * “ means soluble, but s
2、aturation unknown. Mass Solvent Concentration 1 mg5 mg10 mg 1 mM2.4165 mL12.0823 mL24.1645 mL 5 mM0.4833 mL2.4165 mL4.8329 mL 10 mM0.2416 mL1.2082 mL2.4165 mL 制备储备液 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
3、根据储存条 件，适当保存；以下溶剂前的百分是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% saline Solubility: 5 mg/mL (12.08 mM); Clear solution 2. 请依序添加每种溶剂： 10% DMSO 90% corn oil Solubility: 5 mg/mL (12.08 mM); Clear solution 1/3Master of Small Molecules 您边的抑制剂师 www.MedChemE BIOLOGICAL ACTIVITY 物活
4、性 PLX-4720 是种有效的，选择性的 B-RafV600E 抑制剂，IC50 值为 13 nM；与对 c-Raf-1 的选择性相同，是野 型 B-Raf 选择性的 10 倍。 IC50 128(9):3976-3990. Mol Syst Biol. 2015 Mar 26;11(3):797. ACS Chem Biol. 2017 May 19;12(5):1245-1256. See more customer validations on www.MedChemE REFERENCES 1. Tsai J, et al. Discovery of a selective inhi
5、bitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci U S A, 2008, 105(8), 3041-3046. 2. Paraiso KH, et al. PTEN loss confers BRAF inhibitor resistance to melanoma cells through the suppression of BIM expression. Cancer Res, 2011, 71(7), 2750-2760. 3. Nucera C, et al.
6、 B-Raf(V600E) and thrombospondin-1 promote thyroid cancer progression. Proc Natl Acad Sci U S A, 2010, 107(23), 10649-10654. 4. Rizzolio S, et al. Neuropilin-1 upregulation elicits adaptive resistance to oncogene-targeted therapies. J Clin Invest. 2018 Aug 31;128(9):3976-3990. McePdfHeight Caution: Product has not been fully validated for medical applications. For research use only. Tel: 400-820-3792; 021-58955995 Fax: 021-53700325 E-mail: techMedChemE 3/3Master of Small Molecules 您边的抑制剂师
