Lestaurtinib

Lestaurtinib (CEP-701) is an orally active and selective RPTKs (receptor protein tyrosine kinase) inhibitor, competitively inhibits ATP binding to the TrkA/B/C domain. Lestaurtinib inhibits RPTKs phosphorylation, with IC50s of 2, 25 and 0.9 nM for FLT3, TrkA and JAK2, respectively. Lestaurtinib induces apoptosis and cycle arrest, also can inhibit growth of tumor[1][2][3][4][5][6].

Product Specifications

CAS Number

[111358-88-4]

Product Name Alternative

CEP-701; KT-5555

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

Apoptosis; FLT3; JAK; STAT; Trk Receptor

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics; JAK/STAT Signaling; Neuronal Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Lestaurtinib.html

Purity

99.66

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(NC1)C2=C1C3=C(C4=C52)N(C6=C3C=CC=C6)[C@@]([C@@](O)(CO)C7)(C)O[C@H]7N4C8=C5C=CC=C8

Molecular Formula

C26H21N3O4

Molecular Weight

439.46

Precautions

H315, H319, H335

References & Citations

[1]Pinto N, et al. Lestaurtinib is a potent inhibitor of anaplastic thyroid cancer cell line models. PLoS One. 2018 Nov 12;13 (11) :e0207152.|[2]Diaz T, et al. Lestaurtinib inhibition of the Jak/STAT signaling pathway in hodgkin lymphoma inhibits proliferation and induces apoptosis. PLoS One. 2011 Apr 20;6 (4) :e18856. |[3]Iyer R, et al. Lestaurtinib enhances the antitumor efficacy of chemotherapy in murine xenograft models of neuroblastoma. Clin Cancer Res. 2010 Mar 1;16 (5) :1478-85.|[4]Levis M, et al. A FLT3-targeted tyrosine kinase inhibitor is cytotoxic to leukemia cells in vitro and in vivo. Blood. 2002 Jun 1;99 (11) :3885-91.|[5]Shabbir M, et al. Lestaurtinib, a multitargeted tyrosine kinase inhibitor: from bench to bedside. Expert Opin Investig Drugs. 2010 Mar;19 (3) :427-36. |[6]Hexner EO, et al. Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders. Blood. 2008 Jun 15;111 (12) :5663-71.