2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Neuronal Signaling Apoptosis
  3. JAK FLT3 Trk Receptor Apoptosis STAT
  4. Lestaurtinib

Lestaurtinib  (Synonyms: CEP-701; KT-5555)

Cat. No.: HY-50867 Purity: 99.17%
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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.

For research use only. We do not sell to patients.

Lestaurtinib Chemical Structure

Lestaurtinib Chemical Structure

CAS No. : 111358-88-4

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1 mg USD 280 In-stock
5 mg USD 690 In-stock
10 mg USD 1100 In-stock
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Based on 3 publication(s) in Google Scholar

Lestaurtinib Related Antibodies

Top Publications Citing Use of Products

View All JAK Isoform Specific Products:

View All Isoforms
JAK1 JAK2 JAK3 Tyk2 JAK

View All Trk Receptor Isoform Specific Products:

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TrkA TrkB TrkC Trk

View All STAT Isoform Specific Products:

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STAT3 STAT5 STAT6 STAT1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3][4][5][6].

IC50 & Target[1]

JAK2

0.9 nM (IC50)

TrkA

25 nM (IC50)

FLT3

2 nM (IC50)

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.

Lestaurtinib Related Antibodies

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
Molecular Weight

439.46

Formula

C26H21N3O4
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light

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

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2755 mL 11.3776 mL 22.7552 mL
5 mM 0.4551 mL 2.2755 mL 4.5510 mL
View the Complete Stock Solution Preparation Table

* 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.

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.17%

COA (268 KB) LCMS (277 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

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
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Lestaurtinib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lestaurtinib111358-88-4CEP-701 KT-5555CEP701CEP 701KT5555KT 5555KT-5555JAKFLT3Trk ReceptorApoptosisSTATJanus kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Tropomyosin related kinase receptor PDACATChodgkin lymphomaCAL62KMH2Inhibitorinhibitorinhibit

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