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Lestaurtinib

🥰Excellent
Catalog No. T15738Cas No. 111358-88-4
Alias KT-5555, KT5555, KT 5555, CEP-701, CEP701, CEP 701

Lestaurtinib (CEP 701) is an orally available and selective inhibitor of FMS-like tyrosine kinase-3 (FLT3, IC50: 0.9 nM), which inhibits FLT3 autophosphorylation in vitro.Lestaurtinib promotes the expression of c-MYC, inhibits the phosphorylation of RPTKs, and has high affinity for TrkA and JAK2. Lestaurtinib promotes c-MYC expression, inhibits phosphorylation of RPTKs, has a high affinity for TrkA and JAK2, induces apoptosis and cell growth arrest, and can be used to study leukemia.

Lestaurtinib

Lestaurtinib

🥰Excellent
Purity: 99.17%
Catalog No. T15738Alias KT-5555, KT5555, KT 5555, CEP-701, CEP701, CEP 701Cas No. 111358-88-4
Lestaurtinib (CEP 701) is an orally available and selective inhibitor of FMS-like tyrosine kinase-3 (FLT3, IC50: 0.9 nM), which inhibits FLT3 autophosphorylation in vitro.Lestaurtinib promotes the expression of c-MYC, inhibits the phosphorylation of RPTKs, and has high affinity for TrkA and JAK2. Lestaurtinib promotes c-MYC expression, inhibits phosphorylation of RPTKs, has a high affinity for TrkA and JAK2, induces apoptosis and cell growth arrest, and can be used to study leukemia.
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1 mg$499In Stock
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Purity:99.17%
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Product Introduction

Bioactivity
Description
Lestaurtinib (CEP 701) is an orally available and selective inhibitor of FMS-like tyrosine kinase-3 (FLT3, IC50: 0.9 nM), which inhibits FLT3 autophosphorylation in vitro.Lestaurtinib promotes the expression of c-MYC, inhibits the phosphorylation of RPTKs, and has high affinity for TrkA and JAK2. Lestaurtinib promotes c-MYC expression, inhibits phosphorylation of RPTKs, has a high affinity for TrkA and JAK2, induces apoptosis and cell growth arrest, and can be used to study leukemia.
Targets&IC50
TrkA:25 nM, JAK2:0.9 nM, FLT3:3 nM
In vitro
METHODS: Cells were treated with different concentrations of Lestaurtinib (0.5 μM and 4.0 μM) and cell viability was assessed using PrestoBlue at different time points (0, 24, 48, and 72 hours) by measuring the fluorescence intensity to evaluate cell proliferation.
RESULTS: Lestaurtinib demonstrated good proliferative inhibitory activity against the KMH2, CAL62, and THJ-21T cell lines[1].
In vivo
METHODS: Lestaurtinib (20 mg/kg; subcutaneous injection; twice daily from Monday to Friday and once daily on Saturday and Sunday; for 3 weeks) was administered to four-week-old athymic nude mice (SY5Y-TrkB xenograft model) to evaluate its therapeutic effect in a preclinical neuroblastoma model.
RESULTS: Lestaurtinib significantly slowed the growth of SY5Y-TrkB xenografts [3].
AliasKT-5555, KT5555, KT 5555, CEP-701, CEP701, CEP 701
Chemical Properties
Molecular Weight439.46
FormulaC26H21N3O4
Cas No.111358-88-4
SmilesC[C@]12N3C=4C=5N(C=6C(C5C7=C(C4C=8C3=CC=CC8)CNC7=O)=CC=CC6)[C@](O1)(C[C@@]2(CO)O)[H]
Relative Density.1.7g/cm3
Storage & Solubility Information
Storagestore at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 40 mg/mL (91.02 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2755 mL11.3776 mL22.7552 mL113.7760 mL
5 mM0.4551 mL2.2755 mL4.5510 mL22.7552 mL
10 mM0.2276 mL1.1378 mL2.2755 mL11.3776 mL
20 mM0.1138 mL0.5689 mL1.1378 mL5.6888 mL
50 mM0.0455 mL0.2276 mL0.4551 mL2.2755 mL

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