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| Lestaurtinib Basic information |
| Product Name: | Lestaurtinib | | Synonyms: | 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 | | CAS: | 111358-88-4 | | MF: | C26H21N3O4 | | MW: | 439.47 | | EINECS: | | Product Categories: | Inhibitor;Intermediates & Fine Chemicals;Pharmaceuticals | | Mol File: | 111358-88-4.mol |
| Lestaurtinib Chemical Properties |
| 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 |
| WGK Germany | 3 | | HS Code | 2934999090 |
| Lestaurtinib Usage And Synthesis |
| 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
| | 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. | | 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 |
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