| Identification | Back Directory | [Name]
Lestaurtinib | [CAS]
111358-88-4 | [Synonyms]
SP 924
CEP 701
KT 5555
SPM-924
A 154475.0
Apalutamide
lestaurtinib
CEP-701 hydrate
KT-5555 hydrate
Lestaurtinib hydrate
(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
(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 | [Molecular Formula]
C26H21N3O4 | [MDL Number]
MFCD12828858 | [MOL File]
111358-88-4.mol | [Molecular Weight]
439.469 |
| Chemical Properties | Back Directory | [Appearance]
Off-White Solid | [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 |
| Hazard Information | Back Directory | [Chemical Properties]
Off-White Solid | [Uses]
It is used for the treatment of pancreatic cancer and acute myelogenous leukaemia (AML) | [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 . | [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. | [Definition]
ChEBI: LSM-1231 is an indolocarbazole. | [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, protect from light | [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 |
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| Company Name: |
LGM Pharma
|
| Tel: |
1-(800)-881-8210 |
| Website: |
www.lgmpharma.com |
|