Lestaurtinib

Bezeichnung:Lestaurtinib

CAS-Nr111358-88-4

Englisch Name:Lestaurtinib

CBNumberCB3506750

SummenformelC26H21N3O4

Molgewicht439.47

MOL-Datei111358-88-4.mol

Lestaurtinib physikalisch-chemischer Eigenschaften

Schmelzpunkt	215-220°C
Siedepunkt	723.0±60.0 °C(Predicted)
Dichte	1.70±0.1 g/cm3(Predicted)
storage temp.	Desiccate at -20°C
Löslichkeit	DMSO: >10mg/mL
Aggregatzustand	white powder
pka	13.37±0.40(Predicted)
Farbe	White or off-white
Stabilität	Photosensitive

Sicherheit

WGK Germany	3
HS Code	2934999090

Gefahreninformationscode (GHS)

Lestaurtinib Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Chemische Eigenschaften
Lestaurtinib is Off-White Solid
Verwenden
Lestaurtinib is used for the treatment of pancreatic cancer and acute myelogenous leukaemia (AML)
Verwenden
It is used for the treatment of pancreatic cancer and acute myelogenous leukaemia (AML).
Verwenden
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.
Biologische Aktivität
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.
Lager
-20°C (desiccate)
Einzelnachweise
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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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