Lestaurtinib

• Description :

  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 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.

• Shipping Conditions :

  Blue Ice

• Storage Conditions :

  -20°C (Powder, protect from light)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Launched

• Isoform :

  JAK2; TrkA

• CAS Number :

  [111358-88-4]