1. Protein Tyrosine Kinase/RTK
  2. FLT3
  3. Tandutinib

Tandutinib (Synonyms: MLN518; CT53518)

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

Tandutinib (MLN518, CT53518) is a potent FLT3 antagonist with IC50 of 0.22 μM, also inhibits PDGFR and c-Kit, 15 to 20-fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR and KDR.

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
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

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Description

Tandutinib (MLN518, CT53518) is a potent FLT3 antagonist with IC50 of 0.22 μM, also inhibits PDGFR and c-Kit, 15 to 20-fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR and KDR. IC50 value: 0.22 uM [1] Target: Flt3; PDGFRβ; c-Kit in vitro: Tandutinib has little activity against EGFR, FGFR, KDR, InsR, Src, Abl, PKC, PKA and MAPKs. Tandutinib inhibits IL-3-independent cell growth and FLT3-ITD autophosphorylation with an IC50 of 10-100 nM. Tandutinib also inhibits the proliferation of human leukemia Ba/F3 cells containing FLT3-ITD mutations with IC50 values of 10-30 nM, and the FLT3-ITD-positive Molm-13 and Molm-14 cells with an IC50 of 10 nM. In FLT3-ITD-positive Molm-14 cells but not the FLT3-ITD-negative THP-1 cells, Tandutinib treatment leads to significant apoptosis by 51% and 78% at 24 and 96 hours, respectively, due to specific FLT3 inhibition [1]. Tandutinib preferentially inhibits the growth of blast colonies from FLT3 ITD-positive compared with ITD-negative patients with AML, without affecting colony formation by normal human progenitor cells [2]. in vivo: Oral administration of Tandutinib at 60 mg/kg bid significantly increases the survival in mice bearing Ba/F3 cells expressing W51 FLT3-ITD mutant, and gives a significant reduction in mortality in a mouse bone marrow transplantation model [1]. Tandutinib treatment at 180 mg/kg twice daily has mild toxicity toward normal hematopoiesis, however, it is a dose at which Tandutinib is effective in treating FLT3 ITD-positive leukemia in mice [2].

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 : ≥ 36 mg/mL (63.98 mM)

*"≥" means soluble, but saturation unknown.

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.

    Tandutinib is prepared in PBS[4].

References

Purity: 99.81%

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Tandutinib
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