A potent JAK2 and PRK1 kinase inhibitor
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Lestaurtinib

Item No. 12094

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,3,9S,10S,11,12R-hexahydro-10-hydroxy-10-(hydroxymethyl)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one
CAS Number
111358-88-4
Synonyms
  • A 154475.0
  • CEP-701
  • KT 5555
  • NSC 621867
  • SP 924
Molecular Formula
C26H21N3O4
Formula Weight
439.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMF:PBS (pH 7.2) (1:20): 0.05 mg/mlDMSO: 3 mg/ml
λmax
209, 245, 292, 337, 352,369 nm
SMILES
O=C(NC1)C2=C1C(C(C=CC=C3)=C3N45)=C4C6=C2C7=C(C=CC=C7)N6[C@@]8([H])C[C@](O)(CO)[C@]5(C)O8
InChi Code
InChI=1S/C26H21N3O4/c1-25-26(32,12-30)10-18(33-25)28-16-8-4-2-6-13(16)20-21-15(11-27-24(21)31)19-14-7-3-5-9-17(14)29(25)23(19)22(20)28/h2-9,18,30,32H,10-12H2,1H3,(H,27,31)/t18-,25+,26+/m1/s1
InChi Key
UIARLYUEJFELEN-LROUJFHJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

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    Product Description

    Lestaurtinib is a staurosporine analog that potently inhibits JAK2 kinase (IC50 = 1 nM) and downstream targets STAT5 (IC50 = 10-30 nM) and STAT3 in a human erythroleukemic cell line expressing the JAK2V617F mutation.1,2 It has been used to reduce tumor growth in a xenograft model of pancreatic ductal adenocarcinoma, to inhibit cell growth in a trk-B overexpressing neuroblastoma xenograft model, and to block proliferation and induce apoptosis in Hodgkin lymphoma cell lines.3,4,5 Lestaurtinib has since been reported to potently inhibit the epigenetic kinase PRK1 in vitro (IC50 = 8.6 nM), inducing hypophosphorylation of histone H3 threonine 11 and blocking androgen-dependent gene expression in prostate cancer cells at a concentration of 5 μM.6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Verstovsek, S. Therapeutic potential of JAK2 inhibitors. Hematology Am. Soc. Hematol. Educ. Program 636-642 (2009).

    2. Hexner, E.O., Serdikoff, C., Jan, M., 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 111(12), 5663-5671 (2008).

    3. Miknyoczki, S.J., Chang, H., Klein-Szanto, A., et al. The Trk tyrosine kinase inhibitor CEP-701 (KT-5555) exhibits significant antitumor efficacy in preclinical xenograft models of human pancreatic ductal adenocarcinoma. Clin. Cancer Res. 5, 2205-2212 (1999).

    4. Iyer, R., Evans, A.E., Qi, X., et al. Lestaurtinib enhances the anti-tumor efficacy of chemotherapy in murine xenograft models of neuroblastoma. Clin. Cancer Res. 16(5), 1478-1485 (2010).

    5. Diaz, T., Navarro, A., Ferrer, G., et al. Lestaurtinib inhibition of the JAK/STAT signaling pathway in Hodgkin lymphoma inhibits proliferation and induces apoptosis. PLoS One 6(4), (2011).

    6. Köhler, J., Erlenkamp, G., Eberlin, A., et al. Lestaurtinib inhibits histone phosphorylation and androgen-dependent gene expression in prostate cancer cells. PLoS One 7(4), (2012).