RAF709 _Raf 抑制劑 - MedChemExpress

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

2、ng)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產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。體內實驗 請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓膬湟?，再依次添加助溶?為保證實驗結果的可靠性，體內實驗的作液，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，適當保存；以下

3、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: 2.5 mg/mL (4.61 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.61 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.61 mM); Clear so

4、lution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 RAF709種有效的 RAF 抑制劑，抑制 BRAF 和 CRAF，IC50 分別為 0.4 nM 和 0.5 nM 1。具有抗腫瘤活性1。IC50 & Target CRAF Braf0.5 nM (IC50) 0.4 nM (IC50)體外研究 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.體內研究 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.戶使本產品發(fā)表的科研獻 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