Art. -Nr.: HY-50867

Lestaurtinib

(Synonyms: CEP-701; KT-5555)

4 Cited Publications

Kundenbewertung

Based on 4 publication(s) in Google Scholar

Lestaurtinib (CEP-701) is an orally active and selective RPTKs (receptor protein tyrosine kinase) inhibitor, competitively inhibits ATP binding to the TrkA/B/C domain. Lestaurtinib inhibits RPTKs phosphorylation, with IC₅₀s of 2, 25 and 0.9 nM for FLT3, TrkA and JAK2, respectively. Lestaurtinib induces apoptosis and cycle arrest, also can inhibit growth of tumor.

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Reinheit: 99.66%
CAS. Nr.: 111358-88-4
Formel: C₂₆H₂₁N₃O₄
Molecular Weight:439.46

Speicherung:

-20°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lestaurtinib Chemical Structure

CAS. Nr.: 111358-88-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

JAK2

0.9 nM (IC₅₀)

TrkA

25 nM (IC₅₀)

FLT3

2 nM (IC₅₀)

Alle JAK Isoform-spezifische Produkte anzeigen :

Alle Trk Receptor Isoform-spezifische Produkte anzeigen :

Alle STAT Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	32 nM Compound: CEP-701	Toxicity against human A375 cells after 72 hrs by cell titer-blue assay Toxicity against human A375 cells after 72 hrs by cell titer-blue assay	[PMID: 19654408]
BaF3	GI₅₀	<200 nM Compound: 2	Growth inhibition of mouse Baf3 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Growth inhibition of mouse Baf3 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 35923716]
BaF3	GI₅₀	5 nM Compound: 2	Growth inhibition of mouse BAF3 cells harboring FLT3 ITD mutant assessed as reduction in cell inhibition measured after 72 hrs by MTT assay Growth inhibition of mouse BAF3 cells harboring FLT3 ITD mutant assessed as reduction in cell inhibition measured after 72 hrs by MTT assay	[PMID: 35923716]
BaF3	IC₅₀	3 nM Compound: Lestaurtinib	Antiproliferative activity against mouse BaF3 FLT3-ITD cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 FLT3-ITD cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 32659083]
BaF3	IC₅₀	5 nM Compound: Lestaurtinib	Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 32659083]
BFTC-905	CC₅₀	>3 μM Compound: 46; CEP-701, KT-5555	Cytotoxicity against human BFTC-905 cells Cytotoxicity against human BFTC-905 cells	[PMID: 33539089]
MV4-11	GI₅₀	33 nM Compound: Lestaurtinib	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition after 72 hrs by WST assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition after 72 hrs by WST assay	[PMID: 32272419]
MV4-11	IC₅₀	0.009 μM Compound: Lestaurtinib	Antiproliferative activity against wild type FLT3 expressing human MV411 cells after 72 hrs by WST8 assay Antiproliferative activity against wild type FLT3 expressing human MV411 cells after 72 hrs by WST8 assay	[PMID: 20153646]
MV4-11	IC₅₀	2.1 nM Compound: CEP-701	Cytotoxicity against human MV4-11 cells after 72 hrs by cell titer-blue assay Cytotoxicity against human MV4-11 cells after 72 hrs by cell titer-blue assay	[PMID: 19654408]
MV4-11	IC₅₀	2.5 nM Compound: 3	Inhibition of FLT3-mediated STAT5 phosphorylation in human MV411 cells after 1 hr by immunoblotting analysis Inhibition of FLT3-mediated STAT5 phosphorylation in human MV411 cells after 1 hr by immunoblotting analysis	10.1039/C1MD00175B
RS4-11	IC₅₀	0.12 μM Compound: Lestaurtinib	Antiproliferative activity against human RS4:11 cells having FLT3-ITD mutation after 72 hrs by WST8 assay Antiproliferative activity against human RS4:11 cells having FLT3-ITD mutation after 72 hrs by WST8 assay	[PMID: 20153646]
RS4-11	IC₅₀	1.5 nM Compound: CEP-701	Inhibition of FLT3 ITD mutant autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay Inhibition of FLT3 ITD mutant autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay	[PMID: 19654408]
RS4-11	IC₅₀	2.6 nM Compound: CEP-701	Inhibition of FLT3 autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay Inhibition of FLT3 autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay	[PMID: 19654408]

In Vitro

Lestaurtinib (0.01-10 μM; 72 h) inhibits growth of ATC cells, with IC₅₀s of 0.21, 0.41 and 2.35 μM for KMH2, CAL62 and THJ-21T cells, respectively^[1].
Lestaurtinib (0.125-4 μM; 24 h) decreases STAT5 phosphorylation in a concentration-dependent manner, and completely inhibits expression of pSTAT5 at 4 μM^[1].
Lestaurtinib (0.5 μM; 24 h) shows antiproliferative effect on WI-38, CAL62 and KMH2 cells^[1].
Lestaurtinib (4 μM; 24 h) induces cell cycle arrest in the G2/M phase in CAL62 and KMH2 cells^[1].
Lestaurtinib (30-300 nM; 48 h) induces apoptosis in a dose-dependent manner in HL (hodgkin lymphoma) cell lines^[2].
Lestaurtinib (30, 100, 300 nM; 1 h) inhibits JAK2, STAT5 and STAT3 phosphorylation when at 300 nM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

KMH2, CAL62, THJ-21T cells
Concentration:

0.01-10 µM
Incubation Time:

72 h
Result:

Showed good growth inhibitory activity with IC₅₀s of 0.21, 0.41 and 2.35 µM for KMH2, CAL62 and THJ-21T cells, respectively.

Cell Proliferation Assay^[1]

Cell Line:

WI-38, CAL62 and KMH2 cells
Concentration:

0.5 µM
Incubation Time:

24 h
Result:

Inhibited proliferation of ATC cells.

Cell Cycle Analysis^[1]

Cell Line:

CAL62 and KMH2 cells
Concentration:

4 μM
Incubation Time:

24 h
Result:

Led to increase in the number of cells in the G2/M phase, and decrease in the number of cells in the G1/G0 and S phases (KMH2 cells more significant than CAL62 cells).

Western Blot Analysis^[1]

Cell Line:

CAL62 cells
Concentration:

0.125-4 µM
Incubation Time:

24 h
Result:

Decreased pSTAT5 in a concentration-dependent manner, with a complete disappearance of pSTAT5expression at 4 μM.

Apoptosis Analysis^[2]

Cell Line:

L-428, L-1236, L-540, HDLM-2 and HDMY-Z cells
Concentration:

30-300 nM
Incubation Time:

48 h
Result:

Increased apoptosis rate of 62%, 57%, 10%, 64%, 30% for L-428, L-1236, L-540, HDLM-2 and HD-MY-Z cells respectively, when at 300 nM (in a dose-dependent manner).

Western Blot Analysis^[2]

Cell Line:

L-428, L-1236, L-540, HDLM-2 and HD-MY-Z cells
Concentration:

30, 100, 300 nM
Incubation Time:

1 h
Result:

Decreased phospho-JAK2, -STAT5 and -STAT3 levels of all the HL cell lines by 46-94%, 88-100% and 97-100%, respectively (when at 300 nM).

In Vivo

Lestaurtinib (20 mg/kg; s.c.; twice daily (monday to friday) and once daily (saturday and sunday); 3 weeks) significantly inhibits growth of tumor in vivo^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Four-week-old athymic nu/nu mice (SY5Y-TrkB xenografts model)^[3].
Dosage:

20 mg/kg
Administration:

Subcutaneous injection; twice daily (monday to friday) and once daily (saturday and sunday); 3 weeks.
Result:

Significantly slowed the growth of SY5Y-TrkB xenografts.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 111358-88-4
Appearance Solid
Molecular Weight 439.46
Formel C₂₆H₂₁N₃O₄
Color White to off-white
SMILES

O=C(NC1)C2=C1C3=C(C4=C52)N(C6=C3C=CC=C6)[C@@]([C@@](O)(CO)C7)(C)O[C@H]7N4C8=C5C=CC=C8
Synonyms

CEP-701; KT-5555
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (4)

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Journal Impact Factor

Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Mol Syst Biol

Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]

2024 Jan;20(1):28-55. PMID: 38177929
Cancer Cell Int

Construction of a prognostic model with histone modification-related genes and identification of potential drugs in pancreatic cancer. [Abstract]

2021 Jun 5;21(1):291. PMID: 34090418
bioRxiv

Sphingosine-1-phosphate receptor modulators resensitize FLT3-ITD acute myeloid leukemia cells with NRAS mutations to FLT3 inhibitors. [Abstract]

2025 Nov 24:2025.11.21.689510. PMID: 41341164

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (113.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2755 mL

11.3776 mL

22.7552 mL

5 mM

0.4551 mL

2.2755 mL

4.5510 mL

10 mM

0.2276 mL

1.1378 mL

2.2755 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.5 mg/mL (5.69 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (296 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Pinto N, et al. Lestaurtinib is a potent inhibitor of anaplastic thyroid cancer cell line models. PLoS One. 2018 Nov 12;13(11):e0207152. [Content Brief]

[2]. Diaz T, et al. Lestaurtinib inhibition of the Jak/STAT signaling pathway in hodgkin lymphoma inhibits proliferation and induces apoptosis. PLoS One. 2011 Apr 20;6(4):e18856. [Content Brief]

[3]. Iyer R, et al. Lestaurtinib enhances the antitumor efficacy of chemotherapy in murine xenograft models of neuroblastoma. Clin Cancer Res. 2010 Mar 1;16(5):1478-85. [Content Brief]

[4]. Levis M, et al. A FLT3-targeted tyrosine kinase inhibitor is cytotoxic to leukemia cells in vitro and in vivo. Blood. 2002 Jun 1;99(11):3885-91. [Content Brief]

[5]. Shabbir M, et al. Lestaurtinib, a multitargeted tyrosine kinase inhibitor: from bench to bedside. Expert Opin Investig Drugs. 2010 Mar;19(3):427-36. [Content Brief]

[6]. Hexner EO, et al. Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders. Blood. 2008 Jun 15;111(12):5663-71. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2755 mL	11.3776 mL	22.7552 mL	56.8880 mL
	5 mM	0.4551 mL	2.2755 mL	4.5510 mL	11.3776 mL
	10 mM	0.2276 mL	1.1378 mL	2.2755 mL	5.6888 mL
	15 mM	0.1517 mL	0.7585 mL	1.5170 mL	3.7925 mL
	20 mM	0.1138 mL	0.5689 mL	1.1378 mL	2.8444 mL
	25 mM	0.0910 mL	0.4551 mL	0.9102 mL	2.2755 mL
	30 mM	0.0759 mL	0.3793 mL	0.7585 mL	1.8963 mL
	40 mM	0.0569 mL	0.2844 mL	0.5689 mL	1.4222 mL
	50 mM	0.0455 mL	0.2276 mL	0.4551 mL	1.1378 mL
	60 mM	0.0379 mL	0.1896 mL	0.3793 mL	0.9481 mL
	80 mM	0.0284 mL	0.1422 mL	0.2844 mL	0.7111 mL
	100 mM	0.0228 mL	0.1138 mL	0.2276 mL	0.5689 mL

Lestaurtinib

4 Cited Publications

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Lestaurtinib

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

Publications Citing Use of MedChemExpress (MCE) Lestaurtinib

Alle JAK Isoform-spezifische Produkte anzeigen

Alle Trk Receptor Isoform-spezifische Produkte anzeigen

Alle STAT Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lestaurtinib

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

Publications Citing Use of MedChemExpress (MCE) Lestaurtinib

Alle JAK Isoform-spezifische Produkte anzeigen

Alle Trk Receptor Isoform-spezifische Produkte anzeigen

Alle STAT Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lestaurtinib Related Classifications

HY-50867 Related Classifications