A tyrosine kinase inhibitor
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SU 5416

Item No. 13342

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylene]-1,3-dihydro-2H-indol-2-one
CAS Number
204005-46-9
Synonyms
  • NSC 696819
  • Semaxinib
  • Sugen 5416
  • VEGFR 2 Kinase Inhibitor
Molecular Formula
C15H14N2O
Formula Weight
238.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:2): 0.3 mg/mlDMSO: 10 mg/mlEthanol: 0.25 mg/ml
λmax
212, 278, 441 nm
SMILES
O=C1Nc2ccccc2/C\1=C\c1[nH]c(C)cc1C
InChi Code
InChI=1S/C15H14N2O/c1-9-7-10(2)16-14(9)8-12-11-5-3-4-6-13(11)17-15(12)18/h3-8,16H,1-2H3,(H,17,18)/b12-8-
InChi Key
WUWDLXZGHZSWQZ-WQLSENKSSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

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    Product Description

    SU 5416 is a tyrosine kinase inhibitor best known as an inhibitor of the vascular endothelial growth factor receptor (VEGFR2; FLK1/KDR) and a suppressor of tumor vascularization, preventing the growth of multiple tumor types. In addition to inhibiting VEGFR2 (IC50 = 1 μM), SU 5416 also inhibits PDGFR (IC50 = 20 μM), c-Kit (IC50 = 30 nM), RET (IC50 = 170 nM), FLT3 (IC50 = 160 nM), ABL (IC50 = 11 μM), and ALK (IC50 = 1.2 μM).1,2,3 SU 5416 does not inhibit epidermal growth factor or fibroblast growth factor receptor tyrosine kinases (IC50 > 100 μM).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fong, T.A.T., Shawver, L.K., Sun, L., et al. SU5416 is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) that inhibits tyrosine kinase catalysis, tumor vascularization, and growth of multiple tumor types. Cancer Res. 59(1), 99-106 (1999).

    2. Litz, J., Warshamana-Greene, G.S., Sulanke, G., et al. The multi-targeted kinase inhibitor SU5416 inhibits small cell lung cancer growth andangiogenesis, in part by blocking Kit-mediated VEGF expression. Lung Cancer 46(3), 283-291 (2004).

    3. Mologni, L., Sala, E., Cazzaniga, S., et al. Inhibition of RET tyrosine kinase by SU5416. J. Mol. Endocrinol. 37(2), 199-212 (2006).