1022950-46-4Relevant articles and documents
Design, synthesis, and biological evaluation of a series of novel AXL kinase inhibitors
Mollard, Alexis,Warner, Steven L.,Call, Lee T.,Wade, Mark L.,Bearss, Jared J.,Verma, Anupam,Sharma, Sunil,Vankayalapati, Hariprasad,Bearss, David J.
, p. 907 - 912 (2012/01/19)
The receptor tyrosine kinase AXL has emerged in recent years as an potential oncology target due to its overexpression in several types of cancers coupled with its ability to promote tumor growth and metastasis. To identify small molecule inhibitors of AXL, we built a homology model of its catalytic domain to virtually screen and identify scaffolds displaying an affinity for AXL. Further computational and structure-based design resulted in the synthesis of a series of 2,4,5-trisubstitued pyrimidines, which demonstrated potent inhibition of AXL in vitro (IC50 = 19 nM) and strongly inhibited the growth of several pancreatic cell lines.
