An antagonist of PDGFRβ, FLT3, and c-Kit
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Tandutinib

Item No. 12098

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[6-methoxy-7-[3-(1-piperidinyl)propoxy]-4-quinazolinyl]-N-[4-(1-methylethoxy)phenyl]-1-piperazinecarboxamide
CAS Number
387867-13-2
Synonyms
  • CT 53518
  • MLN518
Molecular Formula
C31H42N6O4
Formula Weight
562.7
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 10 mg/mlEthanol: 10 mg/ml
λmax
247, 332 nm
SMILES
O=C(NC1=CC=C(OC(C)C)C=C1)N(CC2)CCN2C3=NC=NC4=C3C=C(OC)C(OCCCN5CCCCC5)=C4
InChi Code
InChI=1S/C31H42N6O4/c1-23(2)41-25-10-8-24(9-11-25)34-31(38)37-17-15-36(16-18-37)30-26-20-28(39-3)29(21-27(26)32-22-33-30)40-19-7-14-35-12-5-4-6-13-35/h8-11,20-23H,4-7,12-19H2,1-3H3,(H,34,38)
InChi Key
UXXQOJXBIDBUAC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    25 mg

    $62

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    50 mg

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    100 mg

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    Product Description

    Tandutinib is a potent antagonist of platelet-derived growth factor receptor β (PDGFRβ), FLT3, and c-Kit (IC50 = 200, 220, and 170 nM, respectively).1 It less potently inhibits macrophage colony-stimulating factor 1 receptor (IC50 = 3.4 µM) and does not significantly inhibit other tyrosine or serine/threonine kinases.1,2 Tandutinib blocks the growth of cells expressing an internal tandem duplication within the juxtamembrane domain of the FLT3 receptor, found in some acute myelogenous leukemia cells.1,3 It also impairs the growth of colon cancer cells through its actions on the c-Kit receptor.4 Tandutinib reverses multidrug resistance in vitro by impairing the efflux activity of the multidrug resistance protein 7.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kelly, L.M., Yu, J.C., Boulton, C.L., et al. CT53518, a novel selective FLT3 antagonist for the treatment of acute myelogenous leukemia (AML). Cancer Cell. 1(5), 421-432 (2002).

    2. Pandey, A., Volkots, D.L., Seroogy, J.M., et al. Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family. J. Med. Chem. 45(17), 3772-3793 (2002).

    3. Griswold, I.J., Shen, L.J., La Rosée, P., et al. Effects of MLN518, a dual FLT3 and KIT inhibitor, on normal and malignant hematopoiesis. Blood 104(9), 2912-2918 (2004).

    4. Ponnurangam, S., Standing, D., Rangarajan, P., et al. Tandutinib inhibits the Akt/mTOR signaling pathway to inhibit colon cancer growth. Mol. Cancer Ther. 12(5), 598-609 (2013).

    5. Deng, W., Dai, C.L., Chen, J.J., et al. Tandutinib (MLN518) reverses multidrug resistance by inhibiting the efflux activity of the multidrug resistance protein 7 (ABCC10). Oncol. Rep. 29(6), 2479-2485 (2013).