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Cat. No. Name Size Price Add Cart
KI1019Lestaurtinib1 mg$330
Lestaurtinib5 mg$1072

Chemical Characteristic

Product NameLestaurtinib
SynonymsCEP701, KT-5555
CAS No.111358-88-4
Molecular Weight 439.46
FormulaC26H21N3O4
Chemical Name(5S,6S,8R)-6-hydroxy-6-(hydroxymethyl)-5-methyl-7,8,14,15-tetrahydro-5H-16-oxa-4b,8a,14-triaza-5,8-methanodibenzo[b,h]cycloocta[jkl]cyclopenta[e]-as-indacen-13(6H)-one
Smilesn12[C@@]3([C@](C[C@H](n4c5c1c(c1c(c5c5ccccc45)C(=O)NC1)c1ccccc21)O3)(CO)O)C
Chemical Structure

Biological activities

Lestaurtinib is a potent and orally available fms-like kinase (FLT3) inhibitor. Lestaurtinib inhibits phosphorylation of FLT3 with an IC50 of 2 to 3 nM.[1] In vitro, lestaurtinib inhibits wild type JAK2 kinase activity with an IC50 of 1 nM. Lestaurtinib inhibits JAK3 with an IC50 of 3 nM. Lestaurtinib inhibits STAT5 activation and other downstream effectors of JAK2/STAT signaling. Lestaurtinib inhibits the growth of HEL92.1.7 cells, which are dependent on mutant JAK2 activity for growth. [2] Lestaurtinib administration at 10 mg/kg s.c. b.i.d. 5 days a week for 21-28 days inhibits tumor growth in a statistically significant manner in Panc-1, AsPc-1, BxPc-3, Colo 357, and MiaPaCa2 s.c. xenografts in athymic nude mice compared with vehicle-treated controls. [3]

Protocols

Lestaurtinib is stored at -20 °C as a 4 mM stock solution in DMSO and diluted with RPMI culture medium immediately prior to use. [1]

References

[1] Knapper S, et al. The effects of lestaurtinib (CEP701) and PKC412 on primary AML blasts: the induction of cytotoxicity varies with dependence on FLT3 signaling in both FLT3-mutated and wild-type cases. Blood. 2006, 108(10): 3494-3503.
[2] 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, 111(12): 5663-5671.
[3] Miknyoczki SJ, 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. 1999, 5(8): 2205-2212.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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