1. Protein Tyrosine Kinase/RTK
  2. FLT3
    c-Kit
    PDGFR
  3. Tandutinib

Tandutinib (Synonyms: MLN518; CT53518)

Cat. No.: HY-10202 Purity: 99.81%
Handling Instructions

Tandutinib (MLN518) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and platelet-derived growth-factor receptor (PDGFR) with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib can be used to treat acute myelogenous leukemia (AML) . Tandutinib has the ability to cross the blood-brain barrier.

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

Tandutinib Chemical Structure

Tandutinib Chemical Structure

CAS No. : 387867-13-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
50 mg USD 60 In-stock
Estimated Time of Arrival: December 31
100 mg USD 96 In-stock
Estimated Time of Arrival: December 31
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Based on 3 publication(s) in Google Scholar

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Description

Tandutinib (MLN518) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and platelet-derived growth-factor receptor (PDGFR) with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib can be used to treat acute myelogenous leukemia (AML) [1][2]. Tandutinib has the ability to cross the blood-brain barrier[3].

IC50 & Target[1]

PDGFR

0.2 μM (IC50)

In Vitro

Tandutinib (0-3 μM; 30 minutes; Ba/F3 cells) treatment inhibits IL-3-independent cell growth and FLT3-ITD autophosphorylation with an IC50 of 10-100 nM in Ba/F3 cells expressing different FLT3-ITD mutants[1].
Tandutinib (1 μM; 24-96 hours; Molm-14 and THP-1 AML cells) treatment induces apoptosis in FLT3-ITD-positive AML cells[1].
In human FLT3-ITD-positive AML cell lines, Tandutinib inhibits FLT3-ITD phosphorylation (IC50 of ~30 nM). As with Erk2, a constitutively high level of Akt phosphorylation is readily detected and is efficiently blocked by pretreatment of the Molm-14 cells with 100-300 nM Tandutinib[1].
Tandutinib inhibits cell proliferation of the FLT3-ITD-positive Molm-13 and Molm-14 with an IC50 of 10 nM. And signaling through the MAP kinase and PI3 kinase pathways[1].

Apoptosis Analysis[1]

Cell Line: Molm-14 and THP-1 AML cells
Concentration: 1 μM
Incubation Time: 24 hours, 48 hours, 72 hours, 96 hours
Result: Induced apoptosis in FLT3-ITD-positive AML cells.

Western Blot Analysis[1]

Cell Line: Ba/F3 cells
Concentration: 0 μM, 0.003 μM, 0.01 μM, 0.03 μM, 0.1 μM, 1 μM and 3 μM
Incubation Time: 30 minutes
Result: In Ba/F3 cells expressing different FLT3-ITD mutants, inhibited IL-3-independent cell growth and FLT3-ITD autophosphorylation.
In Vivo

Tandutinib (60 mg/kg; oral gavage; daily; for 35 days; athymic nude mice) treatment causes a statistically significant increase in survival that was extended on average by 20 days[1].

Animal Model: Athymic nude mice injected with Ba/F3 cells[1]
Dosage: 60 mg/kg
Administration: Oral gavage; daily; for 35 days
Result: Caused a statistically significant increase in survival that was extended on average by 20 days.
Clinical Trial
Molecular Weight

562.70

Formula

C₃₁H₄₂N₆O₄

CAS No.

387867-13-2

SMILES

O=C(N1CCN(C2=C(C(C=C3OCCCN4CCCCC4)=NC=N2)C=C3OC)CC1)NC5=CC=C(OC(C)C)C=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (88.86 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7771 mL 8.8857 mL 17.7715 mL
5 mM 0.3554 mL 1.7771 mL 3.5543 mL
10 mM 0.1777 mL 0.8886 mL 1.7771 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

TandutinibMLN518CT53518MLN 518MLN-518CT 53518CT-53518FLT3c-KitPDGFRCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3SCFRCD117Platelet-derived growth factor receptorAcutemyelogenousleukemiaautophosphorylationMAPPI3FLT3-ITDblood-brainbarrierInhibitorinhibitorinhibit

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