Cat. No. 3395
Alternative Name: CEP-701
Chemical Name: (9S,10S,12R)-2,3,9,10,11,12-Hexahyd
Biological ActivityPotent JAK2, FLT3 and TrkA inhibitor (IC50 values are 0.9, 3 and < 25 nM, respectively). Also inhibits Aurora kinase A and B (IC50 values are 8.1 and 2.3 nM, respectively) and prevents STAT5 phosphorylation (IC50 = 20 - 30 nM). Exhibits antiproliferative activity in vitro (IC50 = 30 - 100 nM in HEL92.1.7 cells) and is effective against myeloproliferative disorders in vivo.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
Hexner et al (2008) Lestaurinib (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. PMID: 17984313.
Weisel et al (2007) Effect of FLT3 inhibition on normal hematopoietic progenitor cells. Ann.N.Y.Acad.Sci. 1106 190. PMID: 17442779.
Miknyoczki et al (1999) The novel Trk receptor tyrosine kinase inhibitor CEP-701 (KT-5555) exhibits antitumor efficacy against human pancreatic carcinoma (Panc1) xenograft growth and in vivo invasiveness. Ann.N.Y.Acad.Sci. 880 252. PMID: 10415871.
Gäbler Cooperative effects of Janus and Aurora kinase inhibition by CEP701 in cells expressing Jak2V617F. J.Cell Mol.Med. 17 265. PMID: 23301855.
If you know of a relevant reference for this product please let us know.
Citations are publications that use Tocris products. Selected citations for Lestaurtinib include:
Rogers and Gahring (2015) Upregulation of Nicotinic Acetylcholine Receptor α4+β2 through a Ligand-Independent PI3Kβ Mechanism That Is Enhanced by TNFα and the Jak2/p38Mapk Pathways. Eur J Neurosci 10 e0143319. PMID: 26619345.
Deshpande et al (2012) Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms. Leukemia 26 708. PMID: 21926964.
Do you know of a great paper that uses Lestaurtinib from Tocris? If so please let us know.
View Related Products by Target
View Related Products by Product Action
Keywords: Lestaurtinib, supplier, TrkA, JAK2, FLT3, inhibitors, inhibits, Neurotrophin, Receptors, Tyrosine, Kinases, RTKs, Janus-Activated, CEP701, aurora, kinases, AurA, AurB, Tocris Bioscience, JAK Kinase Inhibitor products
Find multiple products by catalog number
New Products in this Area
Selective non-ATP competitive inhibitor of GSK 3βBI 605906
Selective IKKβ inhibitorGSK 319347A
Potent and selective IKKε inhibitorFRAX 597
Potent group I PAK inhibitorMRT 68921 dihydrochloride
Potent ULK inhibitor; inhibits autophagyAM 2394
Potent glucokinase activator; orally bioavailableeCF 309
Potent mTOR inhibitorPF 3758309 dihydrochloride
Potent PAK4 inhibitor; orally availableAZ Dyrk1B 33
Potent and selective Dyrk1B kinase inhibitorPF 06409577
Potent and selective allosteric activator of AMPKPerifosine
PKB/Akt inhibitor; also modulates Kv2.1 currentRAF 265
Raf kinase and VEGFR-2 inhibitorCZC 25146
Potent LRRK2 inhibitorRo 3280
Potent and selective PLK1 inhibitorRMM 46
MSK/RSK family kinase inhibitorLTURM 34
Potent DNA-PK inhibitorMLi-2
Potent and selective LRRK2 inhibitorLTURM 36
PI 3-kinase δ inhibitorPI 3065
Potent and selective PI 3-kinase p110δ inhibitorAZ PFKFB3 67
Potent and selective PFKFB3 inhibitorSTOCK2S 26016
Lysine deficient protein kinase (WNK) signaling inhibitor
Follow @Tocris on Twitter
Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.