Ceritinib is an orally available inhibitor of the receptor tyrosine kinase activity of anaplastic lymphoma kinase (ALK) with antineoplastic activity. Upon administration, ceritinib binds to and inhibits wild-type ALK kinase, ALK fusion proteins and ALK point mutation variants. Inhibition of ALK leads to both the disruption of ALK-mediated signaling and the inhibition of cell growth in ALK-overexpressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development. ALK dysregulation and gene rearrangements are associated with a variety of tumor cell types.
色瑞替尼制备储备液:
浓度溶解体积质量
1mg
5mg
10mg
1mM
2.1032mL
10.5159mL
21.0318mL
5mM
0.4206mL
2.1032mL
4.2064mL
10mM
0.2103mL
1.0516mL
2.1032mL
50mM
0.0421mL
0.2103mL
0.4206mL
色瑞替尼临床数据( 数据源于:http:// clinicaltrials.gov)
Conversion of different model animals based on BSA(Value based on data from FDA Draft Guidelines)
Animal A (mg/kg)=Animal B(mg/kg)multiplied by AnimalBm系数/AnimalAm系数 For example, to modify the dose of resveratrol uesd for a mouse(22.4mg/kg) to a dose based on the BSA for a rat, multiply 22.4mg/kg by the Km factor for a mouse and zhen divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2mg/kg