| 产品描述: |                                             Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively. Alectinib demonstrates effective central nervous system (CNS) penetration | 
                                    
                                    	      		      			      				      		
                            | 靶点: | 
                            IC50: 1.9 nM(ALK), 1 nM (ALKF1174L), 3.5 nM (ALKR1275Q)  Kd: 2.4 nM (ALK);VEGFR;TyrosineKinases;ALK | 
                        
	      			      			      			      		
                            | 体内研究: | 
                            Alectinib (0.2-20 mg/kg; oral administration; once daily; for 11 days; SCID or nude mice bearing NCI-H2228 cells) treatment can result in dose-dependent tumor growth inhibition (EC50 of 0.46 mg/kg) and tumor regression. At any dose level, no differences in body weight or gross signs of toxicity are observed[1]  | 
                        
	      			      			      			      			      		
                            | 参考文献: | 
                            1. Sakamoto H, et al. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011, 19(5), 679-690.  2. Gadgeel S, et al. Alectinib versus crizotinib in treatment-naive anaplastic lymphoma kinase-positive (ALK+) non-small-cell lung cancer: CNS efficacy results from the ALEX study. Ann Oncol. 2018 Nov 1;29(11):2214-2222. | 
                        
	      			      			      		
                            | 溶解性: | 
                            DMSO  :  6.2  mg/mL  (12.85  mM;  Need  warming) | 
                        
	      			      			      		
                            | 保存条件: | 
                            -20℃ | 
                        
	      			      			      			      		
                            |  配置溶液浓度参考: | 
                            
                                
                                    
                                     | 
                                    1mg | 
                                    5mg | 
                                    10mg |  
                                    
                                    | 1 mM | 
                                    2.072 ml | 
                                    10.36 ml | 
                                    20.72 ml | 
                                     
                                    
                                    | 5 mM | 
                                    0.414 ml | 
                                    2.072 ml | 
                                    4.144 ml | 
                                     
                                    
                                    | 10 mM | 
                                    0.207 ml | 
                                    1.036 ml | 
                                    2.072 ml | 
                                     
                                    
                                    | 50 mM | 
                                    0.041 ml | 
                                    0.207 ml | 
                                    0.414 ml | 
                                     
                                 
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                    | 注意: | 
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