| 产品描述: | TP-0903 is a potent and selective Axl kinase inhibitor. | 
                                    	      		      			      				      		
                            | 靶点: | Apoptosis;TAM Receptor;Apoptosis;TAMReceptor | 
	      			      			      		
                            | 体外研究: | In pancreatic cancer cells (PSN-1), TP-0903 shows strong antiproliferative activity with IC50 of 6 M. TP-0903 also induces strong G2/M arrest by potently inhibiting Aurora A and B. In CLL B cells from all the patients with CLL, TP-0903 causes a dose-dependent induction of massive apoptosis by targeting phosphorylated Axl, and overcomes CLL BMSC-mediated protection of CLL B cells from apoptosis. | 
	      			      			      		
                            | 体内研究: | In the adult rat hippocampus, the intracerebroventricular administration of SAG (2.5 nM) significantly increases the number of newly generated cells and extends survival of hippocampal cells. [3] In mice, SAG (20 μg/g, i.p.) effectively prevents GC-induced neonatal cerebellar developmental abnormalities. | 
	      			      			      		
                            | 细胞实验: | For cell proliferation assays, 45 μL containing 1000 cells per well are seeded into solid white 384-well plates in appropriate media. The following day, TP-0903 is diluted in serum free growth media to 10x desired concentrations and 5 μL is added to each well. Combined compound and cells are incubated for 96 hours. Following incubation, 40 μL of ATP-Lite solution is added to each well, incubated for an additional 10 minutes at room temperature and luminescence is measured on an microplate reader | 
	      			      			      			      		
                            | 参考文献: | 1. Mollard A, Warner SL, Call LT, Wade ML, Bearss JJ, Verma A, Sharma S, Vankayalapati H, Bearss DJ.  Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors. ACS Med Chem Lett. 2011 Dec 8;2(12):907-912.  2. Sinha S, et al. Targeted Axl Inhibition Primes Chronic Lymphocytic Leukemia B Cells to Apoptosis and Shows Synergistic/Additive Effects in Combination with BTK Inhibitors. Clin Cancer Res. 2015, 21(9), 2115-2126. | 
	      			      			      		
                            | 溶解性: | soluble  in  DMSO | 
	      			      			      		
                            | 保存条件: | -20℃ | 
	      			      			      			      		
                            | 配置溶液浓度参考: | 
                                    
                                    |  | 1mg | 5mg | 10mg |  
                                    | 1 mM | 1.938 ml | 9.689 ml | 19.378 ml |  
                                    | 5 mM | 0.388 ml | 1.938 ml | 3.876 ml |  
                                    | 10 mM | 0.194 ml | 0.969 ml | 1.938 ml |  
                                    | 50 mM | 0.039 ml | 0.194 ml | 0.388 ml |  | 
	      		                                
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