c-Kit-IN-1 _c-Kit 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEc-Kit-IN-1Cat. No.: HY-15240CAS No.: 1225278-16-9分式: CHFNO分量: 489.47作靶点: c-Kit; c-Met/HGFR作通路: Protein Tyrosine Kinase/RTK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 (204.30 m

2、M)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.0430 mL 10.2151 mL 20.4303 mL5 mM 0.4086 mL 2.0430 mL 4.0861 mL10 mM 0.2043 mL 1.0215 mL 2.0430 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

3、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 (5.11 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 (5.11 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/

4、2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (5.11 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 c-Kit-IN-1种有效的 c-Kit 和 c-Met 抑制剂，IC50 值 200 nM。IC50 & Target IC50: 1体外研究 c-Kit-IN-1 is a c-Kit and c-Met inhibitor extracted from patent 2010051373A1, compound example 45, has anIC50

5、of 50s of 1.PROTOCOLKinase Assay 1 Activity of c-KIT kinase is determined by following the production of ADP from the kinase reaction throughcoupling with the pyruvate kinase/lactate dehydrogenase system. In this assay, the oxidation of NADH (thusthe decrease at A340nm) is continuously monitored spe

6、ctrophometrically. The reaction mixture (100 L)contained c-KIT (cKIT residues T544-V976, from ProQinase, 5.4 nM), polyE4Y (1 mg/mL), MgC12 (10 mM),pyruvate kinase (4 units), lactate dehydrogenase (0.7 units), phosphoenol pyruvate (1 mM), and NADH (0.28mM) in 90 mM Tris buffer containing 0.2 % octyl-

7、glucoside and 1% DMSO, pH 7.5. Test compounds (e.g., c-Kit-IN-1) are incubated with c-KIT and other reaction reagents at 22C for 50 values are calculated from aseries of percent inhibition values determined at a range of inhibitor concentrations using software routinesas implemented in the GraphPad

8、Prism software package 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 A serial dilution of test compounds (e.g., c-Kit-IN-1) are dispensed into a 96-well black clear bottom plate. Foreach cell line, five thousand cells are added per well

9、 in 200 L complete growth medium. Plates areincubated for 67 hours at 37 degrees Celsius, 5% CO2, 95% humidity. At the end of the incubation period 40L of a 440 M solution of resazurin in PBS is added to each well and incubated for an additional 5 hours at37 degrees Celsius, 5% CO2, 95% humidity. Pl

10、ates are read on a Synergy2 reader using an excitation of 540nM and an emission of 600 nM. Data is analyzed using Prism software to calculate IC50 values 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Daniel L. Flynn, et al. Cyclopropane amides and analogs exhibiting anti-cancer and anti-proliferative activities. WO 2010051373 A1McePdfHeightCaution: Product has not been fully