Lestaurtinib (CEP701)

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 disorders4. Potent Trk inhibitor [5]. Cell permeable.

References:

1) Levis et al. (2003), Novel FLT3 tyrosine kinase inhibitors;  Expert Opin. Investig. Drugs, 12 1951

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