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Lestaurtinib

Name: Lestaurtinib
Brand: TargetMol
SKU: T15738
Price: 228 USD
Availability: InStock
Rating: 5 (10 reviews)

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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

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Purity: 99.17%

Catalog No. T15738Alias KT-5555, KT5555, KT 5555, CEP-701, CEP701, CEP 701Cas No. 111358-88-4

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
1 mg	$228	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Batch Information

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Purity:99.17%

Appearance:Solid

Color:Yellow

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COA LCMS

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	JAK2:0.9 nM, TrkA:25 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].
Synonyms	KT-5555, KT5555, KT 5555, CEP-701, CEP701, CEP 701

Chemical Properties

Molecular Weight	439.46
Formula	C₂₆H₂₁N₃O₄
Cas No.	111358-88-4
Smiles	C[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

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/Shipping at ambient temperature.

Solubility Information

DMSO: 40 mg/mL (91.02 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.55 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2755 mL	11.3776 mL	22.7552 mL	113.7760 mL
5 mM	0.4551 mL	2.2755 mL	4.5510 mL	22.7552 mL
10 mM	0.2276 mL	1.1378 mL	2.2755 mL	11.3776 mL
20 mM	0.1138 mL	0.5689 mL	1.1378 mL	5.6888 mL
50 mM	0.0455 mL	0.2276 mL	0.4551 mL	2.2755 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc