Lestaurtinib
FLT3/ TrkA inhibitor / Potent and selective FLT3 inhibitor (IC50= 2 nM)1,2. Inhibits RET and RET phosphorylation in medullary thyroid carcinoma cells3. Suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders4. Potent Trk inhibitor5. Cell permeable.
Biochemicals & reagents
111358-88-4
KT5555; CEP-701
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
-20°C
TARGET: Kinase -- PATHWAY: Neurotrophin; Proliferation; JAK/STAT -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Cancer