Lestaurtinib
Synonym(s):KT-5555 hydrate;Lestaurtinib hydrate
- CAS NO.:111358-88-4
- Empirical Formula: C26H21N3O4
- Molecular Weight: 439.47
- MDL number: MFCD09840836
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-05-11 20:10:50
What is Lestaurtinib?
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
The Uses of Lestaurtinib
Lestaurtinib is used for the treatment of pancreatic cancer and acute myelogenous leukaemia (AML)
The Uses of Lestaurtinib
It is used for the treatment of pancreatic cancer and acute myelogenous leukaemia (AML).
The Uses of Lestaurtinib
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
What are the applications of Application
Lestaurtinib is a JAK2, FLT3, and TrkA inhibitor
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
Properties of Lestaurtinib
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 |
Safety information for Lestaurtinib
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P271:Use only outdoors or in a well-ventilated area. P280:Wear protective gloves/protective clothing/eye protection/face protection. |
Computed Descriptors for Lestaurtinib
New Products
(R)-3-Aminobutanenitrile Hydrochloride 4-Aminotetrahydropyran-4-carbonitrile Hydrochloride 4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID HCL 4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID 1,4-Dioxa-8-azaspiro[4.5]decane 5-Bromo-2-nitropyridine SODIUM AAS SOLUTION ZINC AAS SOLUTION BUFFER SOLUTION PH 10.0(BORATE) GOOCH CRUCIBLE SINTERED AQUANIL 5 BERYLLIUM AAS SOLUTION XANTHAN GUM Racecadotril SODIUM VALPROATE Diclofenac Sodium Methylcobalamin (vitamin B12) SODIUM METHYL PARABEN Folic Acid Impurity G Dabigatran Acyl-O2-D-Glucuronide Trifluoroacetic Acid Salt Glycopyrronium Bromide EP Impurity I Eltrombopag N-Oxide Impurity Di-Nitroso Acyclovir Impurity K DLRD N-OxideRelated products of tetrahydrofuran
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