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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

J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
Advantage
76
3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801 18930552037
Fax
86-21-50328109
Email
3bsc@sina.com
Country
China
ProdList
15848
Advantage
69
LGM Pharma
Tel
1-(800)-881-8210
Fax
615-250-9817
Email
inquiries@lgmpharma.com
Country
United States
ProdList
2127
Advantage
70
Chemsky(shanghai)International Co.,Ltd.
Tel
021-50135380
Email
shchemsky@sina.com
Country
China
ProdList
32344
Advantage
50
BOC Sciences
Tel
1-631-485-4226; 16314854226
Email
info@bocsci.com
Country
United States
ProdList
14059
Advantage
65
NCE Biomedical Co.,Ltd.
Tel
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax
+86-27-87599188
Country
China
ProdList
1494
Advantage
55
Shanghai Witofly Chemical Co.,Ltd
Tel
Email
sales@witofly.com
Country
China
ProdList
2867
Advantage
52
Shanghai Yolne Chemical Co., Ltd.
Tel
021-62960152
Fax
021-52212593
Email
934678158@qq.com
Country
China
ProdList
9906
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55
TargetMol Chemicals Inc.
Tel
021-33632979 15002134094
Fax
021-33632979
Email
marketing@targetmol.com
Country
China
ProdList
7934
Advantage
58
Jinan Mingya Medical Technology Co., Ltd.
Tel
0531-85828981
Fax
+86-531-85806006
Email
864598798@qq.com
Country
China
ProdList
588
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58
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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:


  • 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