FGFR4-IN-1 - FGFR 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEFGFR4-IN-1Cat. No.: HY-100631CAS No.: 1708971-72-5分式: CHNO分量: 493.52作靶點(diǎn): FGFR作通路: Protein Tyrosine Kinase/RTK儲(chǔ)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(shí)驗(yàn) DMSO : 6.4 mg/mL (12.97 mM; Need warmin

2、g)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.0263 mL 10.1313 mL 20.2626 mL5 mM 0.4053 mL 2.0263 mL 4.0525 mL10 mM 0.2026 mL 1.0131 mL 2.0263 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 FGFR4-IN-1是有效的 FGFR4 抑制劑，IC50 值為 0.7 nM。IC50 & Target FGFR40.7 nM (IC50)體外研究 FGF

3、R4-IN-1 significantly inhibits the proliferation of HuH-7 hepatocellular carcinoma cells with IC50 of 7.8nM 1.1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEPROTOCOLKinase Assay 1 250000 BaF3-Tel-FGFR4 cells per well are seeded in 96-well tissue culture plates in 40 L of growth mediumsupplemented

4、with 10% foetal calf serum, 10 mM HEPES, 1 mM Sodium Pyruvate, 2 mM Stable Glutamineand 1x Penicillin-Streptomycin. Using a liquid handling device, serial 3-fold dilutions of compounds areprepared in DMSO, prediluted in growth medium, followed by transfer of 10 L/well to the cell plates. Afterincuba

5、tion for 1 hour at 37C/5% CO2, 50 L of lysis buffer (150 mM NaCl, 20 mM Tris (pH 7.5), 1 mMEDTA, 1 mM EGTA, 1 % Triton X-100, 10 mM NaF, complements with protease inhibitors and phosphatase)inhibitors is added and incubated for 30 minutes on ice with shaking at 300 rpm. Sample plates are thenfrozen

6、and stored at 70C. Following thawing on ice, the sample plates are centrifuged for 15 minutes at1200 rpm at 6C.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 Methylene blue staining proliferation assay (MBS): The effect of compounds on cel

7、l proliferation is assessedusing HuH-7 hepatocellular carcinoma cells are cultured in the vendor-recommended medium, 10% foetalcalf serum, 1 mM sodium pyruvate, 1x Penicillin/Streptomycin at 37C in a humidified 5% CO2 incubator.Specifically, 5000 cells/well are seeded in 96-well tissue culture plate

8、s in a total media volume of 100 L/welland increasing compound dilutions or DMSO are added 24 hours thereafter in triplicates. 72 hours aftercompound addition, cells are fixed by adding 25 and incubated for 10 minutes at room temperature. Cells arewashed three times with H2O. Cells are washed 3 time

9、s with H2O, 200 mL/well and then lysed by adding200 mL/well of 3% HCl for 30 minutes at room temperature with shaking. Optical density is measured atA650 nm. The concentration of compound providing 50% of proliferation inhibition with respect to DMSO-treated cells is determined (IC50) using XLFit software.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors. WO 2015059668 A1McePdfHeightCaution: Product has not been fully validated