产品描述:
Human anaplastic lymphoma kinase (ALK) is an oncogene that is amplified in neuroblastomas and when juxtaposed with various fusion partners, its constitutive kinase activity is associated with the development of a type of anaplastic large cell lymphoma (ALCL).{29085,29086} TAE684 is an ALK inhibitor that blocks the proliferation of ALCL-derived and ALK-dependent cell lines with IC50 values of 2-5 nM.{29085} When tested against a panel of 35 cells transformed by various tyrosine kinases, TAE684 demonstrated 100- to 1,000-fold selectivity for inhibiting ALK-driven cell proliferation.{29085} TAE684 treatment induces cell cycle arrest and apoptosis in ALK-dependent cell lines and has been used to suppress tumor growth in in vivo models of ALK-positive ALCL and neuroblastoma.{29085,29086} TAE684 is also reported to inhibit the activity of the Parkinson’s disease-linked leucine-rich repeat kinase 2 (IC50s = 7.8 and 6.1 nM for wild-type and G2019S mutant LRRK2, respectively).{29087}