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HomeProduct name listLestaurtinib

Lestaurtinib

Synonym(s):KT-5555 hydrate;Lestaurtinib hydrate

Lestaurtinib Structural

What is Lestaurtinib?

Description

Lestaurtinib (111358-88-4) is a potent and selective FLT3 inhibitor (IC50= 2 nM).1,2?Inhibits RET and RET phosphorylation in medullary thyroid carcinoma cells.3?Suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders.4?Potent Trk inhibitor.5?Cell permeable.

Chemical properties

Lestaurtinib is Off-White Solid

The Uses of Lestaurtinib

Lestaurtinib is used for the treatment of pancreatic cancer and acute myelogenous leukaemia (AML)

The Uses of Lestaurtinib

It is used for the treatment of pancreatic cancer and acute myelogenous leukaemia (AML).

The Uses of Lestaurtinib

CEP-701 hydrate has been used as a tyrosine kinase inhibitor:

  • to study its effects on early growth response protein (EGR) genes and nerve growth factor (NGF) stimulation in human epithelial cells
  • as a supplement in reservoir solution for co-crystallization studies with human receptor-interacting?protein kinase?4 (RIPK4)
  • as an FMS-like tyrosine kinase 3 (FLT3) inhibitor-gold nanoparticle conjugate to study its effects on acute myeloid leukemia

What are the applications of Application

Lestaurtinib is a JAK2, FLT3, and TrkA inhibitor

Definition

ChEBI: LSM-1231 is an indolocarbazole.

Biological Activity

Potent JAK2, FLT3 and TrkA inhibitor (IC 50 values are 0.9, 3 and < 25 nM respectively) that prevents STAT5 phosphorylation (IC 50 = 20 - 30 nM). Exhibits antiproliferative activity in vitro (IC 50 = 30 - 100 nM in HEL92.1.7 cells) and is effective against myeloproliferative disorders in vivo .

Biochem/physiol Actions

CEP-701 hydrate, also known as Lestaurtinib, can repress Janus kinase 2/signal transducer and activator of transcription 5 (JAK2/STAT5) signaling by the specific inhibition of JAK2.

storage

-20°C (desiccate)

References

1) Levis?et al. (2003),?Novel FLT3 tyrosine kinase inhibitors; Expert Opin. Investig. Drugs,?12?1951 2) Chen?et al.?(2005),?FLT3/ITD Mutation Signaling Includes Suppression of SHP-1; J. Biol. Chem.,?280?5361 3) Strock?et al. (2003),?CEP-701 and CEP-751 Inhibit Constitutively Activated RET Tyrosine Kinase Activity and Block Medullary Thyroid Carcinoma Cell Growth; Cancer Res.,?63?5559 4) Hexner?et al. (2008),?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?5663 5) Ruggeri?et al. (1999),?Role of neurotrophin-trk interactions in oncology: the anti-tumor efficacy of potent and selective trk tyrosine kinase inhibitors in pre-clinical tumor models; Curr. Med. Chem.,?6?845

Properties of Lestaurtinib

Melting point: 215-220°C
Boiling point: 723.0±60.0 °C(Predicted)
Density  1.70±0.1 g/cm3(Predicted)
storage temp.  Desiccate at -20°C
solubility  DMSO: >10mg/mL
form  white powder
pka 13.37±0.40(Predicted)
color  White or off-white
Stability: Photosensitive

Safety information for Lestaurtinib

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P271:Use only outdoors or in a well-ventilated area.
P280:Wear protective gloves/protective clothing/eye protection/face protection.

Computed Descriptors for Lestaurtinib

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