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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDubermatinibCat. No.: HY-12963CAS No.: 1341200-45-0Synonyms: TP-0903分式: CHClNOS分量: 516.06作靶点: TAM Receptor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 : 30

2、mg/mL (58.13 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.9378 mL 9.6888 mL 19.3776 mL5 mM 0.3876 mL 1.9378 mL 3.8755 mL10 mM 0.1938 mL 0.9689 mL 1.9378 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。BIOLOGICAL ACTIVITY物活性 Dubermatinib (TP-0903)具有效性和

3、选择性的Axl受体酪氨酸激酶抑制剂,IC50值为27 nM。IC50 & Target IC50: 27nM (Axl) 1体外研究Dubermatinib (TP-0903) displays a potent activity against AXL with an IC50 of 0.027 M. Dubermatinib (TP-1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE0903) shows extremely potent activity in cell viability assays with an IC50 of 6

4、nM against the pancreaticcancer cell line PSN-1. Dubermatinib (TP-0903) is evaluated for its ability to block GAS6-mediated activationof AXL in pancreatic cancer cells. PSN-1 cells are serum-starved and then stimulated with GAS6 in thepresence of various concentrations of TP-0903 1.PROTOCOLCell Assa

5、y 1 For cell proliferation assays, 45 L containing 1000 cells per well are seeded into solid white 384-well platesin appropriate media. The following day, Dubermatinib (TP-0903) is diluted in serum free growth media to10 x desired concentrations and 5 L is added to each well. Combined compound and c

6、ells are incubated for96 hours. Following incubation, 40 L of ATP-Lite solution is added to each well, incubated for an additional10 minutes at room temperature and luminescence is measured on an microplate reader 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Mollard A, et al. Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors. ACS Med Chem Lett. 2011 Dec8;2(12):907-912.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use onl

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