| Name | Lestaurtinib |
| 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. |
| 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]. |
| Storage | store 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.
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| Keywords | Trkreceptor | TrkA | Trk receptor | Lestaurtinib | JAK2 | FLT3 | Apoptosis |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Flubendazole | Cysteamine hydrochloride | Myricetin | Dextran sulfate sodium salt (MW 4500-5500) | Sodium 4-phenylbutyrate | L-Ascorbic acid | L-Glutamic acid | Tributyrin | L-Ascorbic acid sodium salt | Alginic acid |
United States
