Lestaurtinib

Names

[ Name ]:
Lestaurtinib

[Synonym ]:
SP 924
Lestaurtinib
KT 5555
CEP-701 hydrate
CEP-701
(15S,16S,18R)-16-Hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1.0.0.0.0.0]octacosa-1,6,8,10,12,20,22,24,26-nonaen-3-one
UNII-DO989GC5D1
6,9-Epoxy-15H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocin-15-one, 6,7,8,9,16,17-hexahydro-7-hydroxy-7-(hydroxymethyl)-6-methyl-, (6S,7S,9R)-

Biological Activity

[Description]:

Lestaurtinib (CEP-701;KT-5555) is a multi-kinase inhibitor with potent activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA with IC50s of 0.9, 3 and less than 25 nM, respectively.

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> JAK

Signaling Pathways >> Epigenetics >> JAK

Signaling Pathways >> Stem Cell/Wnt >> JAK

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FLT3

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Trk Receptor

[Target]

JAK2:0.9 nM (IC50)

TrkA:25 nM (IC50)

FLT3:3 nM (IC50)

[References]

[1]. Miknyoczki SJ, et al. 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. 1999 Jun 30;880:252-62.

Chemical & Physical Properties

[ Density]:
1.7±0.1 g/cm3

[ Boiling Point ]:
723.0±60.0 °C at 760 mmHg

[ Melting Point ]:
215-220ºC

[ Molecular Formula ]:
C₂₆H₂₁N₃O₄

[ Molecular Weight ]:
439.463

[ Flash Point ]:
391.0±32.9 °C

[ Exact Mass ]:
439.153198

[ PSA ]:
88.65000

[ LogP ]:
3.37

[ Vapour Pressure ]:
0.0±2.5 mmHg at 25°C

[ Index of Refraction ]:
1.880

[ Storage condition ]:
Desiccate at -20°C

[ Stability ]:
Photosensitive

[ Water Solubility ]:
DMSO: >10mg/mL

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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