RAF709 _Raf 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERAF709Cat. No.: HY-100510CAS No.: 1628838-42-5分式: CHFNO分量: 542.55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 : 100 mg/mL (184.31 mM; Need ultrasonic and warmi

2、ng)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.8431 mL 9.2157 mL 18.4315 mL5 mM 0.3686 mL 1.8431 mL 3.6863 mL10 mM 0.1843 mL 0.9216 mL 1.8431 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，适当保存；以下

3、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 (4.61 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 (4.61 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.61 mM); Clear so

4、lution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 RAF709种有效的 RAF 抑制剂，抑制 BRAF 和 CRAF，IC50 分别为 0.4 nM 和 0.5 nM 1。具有抗肿瘤活性1。IC50 & Target CRAF Braf0.5 nM (IC50) 0.4 nM (IC50)体外研究 RAF709 stabilizes BRAF-CRAF dimers with an EC50 of 0.8 M. In cellular assays, the dose-response o

5、fpMEK and pERK are measured in Calu-6 cells with EC50=0.02 and 0.1 M with minimal paradoxicalactivation and inhibition of proliferation with EC50=0.95 M 1.体内研究 RAF709 proves to be soluble, kinase selective, and efficacious in a KRAS mutant xenograft model. RAF709shows dose-proportional increases in

6、plasma exposure and a corresponding dosedependent inhibition ofpERK in Calu-6 tumors. Treatment with RAF709 results in dose-dependent antitumor activity with 10 mg/kgbeing subefficacious (%T/C=92%), 30 mg/kg results in measurable antitumor activity (%T/C=46%), and 200mg/kg results in mean tumor regr

7、ession of 92%, while the same high dose is not efficacious in the PC3,KRAS WT model 1.户使本产品发表的科研献 Proc Natl Acad Sci U S A. 2019 Feb 1.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Nishiguchi GA, et al. Design and Discovery of N-(2-Methyl-5-morpholino-6-(tetrahydro-2H-pyran-4-yl)oxy)-3,3-bipyridin-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers. J Med Chem.2017 Jun 22;60(12):4869-4881.McePdfHeightCaution: Product has not been fully validated for medical applications.For