ChemicalBook > CAS DataBase List > Lestaurtinib

Lestaurtinib

Product Name
Lestaurtinib
CAS No.
111358-88-4
Chemical Name
Lestaurtinib
Synonyms
SP 924;SPM-924;CS-1165;CEP 701;KT 5555;ritatinib; A 154475.0;lestaurtinib;KT-5555 hydrate;CEP-701 hydrate
CBNumber
CB3506750
Molecular Formula
C26H21N3O4
Formula Weight
439.47
MOL File
111358-88-4.mol
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Lestaurtinib Property

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
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Safety

WGK Germany 
3
HS Code 
2934999090
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
C7869
Product name
CEP-701 hydrate
Purity
≥98% (HPLC)
Packaging
1mg
Price
$187
Updated
2024/03/01
Sigma-Aldrich
Product number
C7869
Product name
CEP-701 hydrate
Purity
≥98% (HPLC)
Packaging
5mg
Price
$727
Updated
2024/03/01
Cayman Chemical
Product number
12094
Product name
Lestaurtinib
Purity
≥98%
Packaging
500μg
Price
$44
Updated
2024/03/01
Cayman Chemical
Product number
12094
Product name
Lestaurtinib
Purity
≥98%
Packaging
1mg
Price
$70
Updated
2024/03/01
Cayman Chemical
Product number
12094
Product name
Lestaurtinib
Purity
≥98%
Packaging
5mg
Price
$151
Updated
2024/03/01
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Lestaurtinib Chemical Properties,Usage,Production

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

Uses

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

Uses

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

Uses

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

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

Lestaurtinib Preparation Products And Raw materials

Raw materials

Preparation Products

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Lestaurtinib Suppliers

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View Lastest Price from Lestaurtinib manufacturers

Qiuxian Baitai New Material Co., LTD
Product
Larotrectinib 111358-88-4
Price
US $1.30/g
Min. Order
1g
Purity
99%
Supply Ability
500ton/Month
Release date
2021-10-29
Dideu Industries Group Limited
Product
Lestaurtinib 111358-88-4
Price
US $1.10/g
Min. Order
1g
Purity
99.9%
Supply Ability
100 Tons Min
Release date
2021-07-06

111358-88-4, LestaurtinibRelated Search:

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  • Lestaurtinib (KT-5555
  • CS-1165
  • lestaurtinib
  • (9S-(9α,10β,12α))-2,3,9,10,11,12-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
  • SPM-924
  • CEP-701 hydrate
  • KT-5555 hydrate
  • Lestaurtinib hydrate
  • (15S,16S,18R)-16-HYDROXY-16-(HYDROXYMETHYL)-15-METHYL-28-OXA-4,14,19-TRIAZAOCTACYCLO[12.11.2.1^{15,18}.0^{2,6}.0^{7,27}.0^{8,13}.0^{19,26}.0^{20,25}]OCTACOSA-1(26),2(6),7(27),8,10,12,20,22,24-NONAEN-3-ONE
  • A 154475.0
  • (9S,10S,12R)-2,3,9,10,11,12-Hexahydro-10-hydroxy-10-(hydroxymethyl)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:321kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one
  • CEP 701
  • KT 5555
  • SP 924
  • LESTAURTINIB (CEP-701;KT-5555)
  • 9,12-Epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one, 2,3,9,10,11,12-hexahydro-10-hydroxy-10-(hydroxymethyl)-9-methyl-, (9S,10S,12R)-
  • KT5555-Lestaurtinib
  • Lestaurtinib USP/EP/BP
  • ritatinib
  • 111358-88-4
  • C26H21N3O4
  • Inhibitor
  • Intermediates & Fine Chemicals
  • Pharmaceuticals