Lestaurtinib (111358-88-4) is a potent and selective FLT3 inhibitor (IC50= 2 nM).1,2 Inhibits RET and RET phosphorylation in medullary thyroid carcinoma cells.3 Suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders.4 Potent Trk inhibitor.5 Cell permeable.
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2) Chen et al. (2005), FLT3/ITD Mutation Signaling Includes Supression of SHP-1; J. Biol. Chem., 280 5361
3) Strock et al. (2003), CEP-701 and CEP-751 Inhibit Constitutively Activated RET Tyrosine Kinase Activity and Block Medullary Thyroid Carcinoma Cell Growth; Cancer Res., 63 5559
4) Hexner et al. (2008), Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders; Blood, 111 5663
5) Ruggeri et al. (1999), Role of neurotrophin-trk interactions in oncology: the anti-tumor efficacy of potent and selective trk tyrosine kinase inhibitors in pre-clinical tumor models; Curr. Med. Chem., 6 845