ZM-336372 - Raf 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEZM 336372Cat. No.: HY-13343CAS No.: 208260-29-1分式: CHNO分量: 389.45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 : 50 mg/mL (128.39 mM; Need ultrasonic)H2O : 40%

2、PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.42 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 (6.42 mM); Suspended solution; Need ultrasonic3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (

3、6.42 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 ZM 336372種有效的蛋激酶 c-Raf 抑制劑。在含有 0.1 mM ATP 的情況下，IC 50 值為 0.07 M。IC50 & Target c-Raf0.07 M (IC50, 0.1 mM ATP)體外研究 ZM 336372 is a potent inhibitor of human c-Raf. The IC50 value is 0.07 M in the standard assay, whichcontains 0.1 mM ATP. The IC50, decreases

4、 to 0.01M at 0.025 mM ATP and increases to 0.9 M at 2.5 mMATP indicating that ZM 336372 is a competitive inhibitor with respect to ATP. ZM 336372 inhibits c-Raftenfold more potently than B-Raf 1. Cell proliferation analysis of ZM336372. 3,4-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide

5、growth assay of H727 and BON treated as control, DMSO, and 100 MZM336372 to days 16 and 10, respectively. Both H727 and BON cell proliferation is inhibited in the presenceof drug compared with controls. H727 cells treated with ZM336372 are growth suppressed, whereas controltreatments have significan

6、tly more growth by day 6, continuing up to 16 days. A similar response is also seenin BON cells as growth suppression occurred as early as day 4 and was maintained out to day 10 2.PROTOCOLCell Assay 2 Proliferation of H727 and BON cells after treatment with ZM336372 is measured using a 3,4-(4,5-dime

7、thylthiazol-2-yl)-2,5-diphenyltetrazolium bromide. Cells are trypsinized and plated in triplicate to 24-wellplates and allowed to adhere overnight. Then, cells are treated with either 100 M ZM336372 or DMSO (2%)and incubated. Media are changed every 2 days with new treatment. At each time point, cel

8、l growth rates areanalyzed after the addition of 3,4-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide reagent to thecultured cells. Absorbance is determined using spectrophotometer at a wavelength of 540 nm 2.MCE has not independently confirmed the accuracy of these methods. They are for r

9、eference only.REFERENCES1. Hall-Jackson CA, et al. Paradoxical activation of Raf by a novel Raf inhibitor. Chem Biol. 1999 Aug;6(8):559-68.2. Van Gompel JJ, et al. ZM336372, a Raf-1 activator, suppresses growth and neuroendocrine hormone levels in carcinoid tumor cells. MolCancer Ther. 2005 Jun;4(6):910-7.McePdfHeightCaution: Product has not been fully validated for medic