An inhibitor of select receptor tyrosine kinases
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SU 6668

Item No. 13873

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[(1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-propanoic acid
CAS Number
252916-29-3
Synonyms
  • NSC 702827
  • Orantinib
  • TSU-68
Molecular Formula
C18H18N2O3
Formula Weight
310.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMF:PBS(pH 7.2)(1:1): 0.50 mg/mlDMSO: 2.5 mg/ml
λmax
212, 279, 447 nm
SMILES
O=C1NC2=CC=CC=C2/C1=C/C3=C(C)C(CCC(O)=O)=C(C)N3
InChi Code
InChI=1S/C18H18N2O3/c1-10-12(7-8-17(21)22)11(2)19-16(10)9-14-13-5-3-4-6-15(13)20-18(14)23/h3-6,9,19H,7-8H2,1-2H3,(H,20,23)(H,21,22)/b14-9-
InChi Key
NHFDRBXTEDBWCZ-ZROIWOOFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $35

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    Product Description

    SU 6668 is an inhibitor of the receptor tyrosine kinases PDGFRβ, VEGFR2, and FGFR1 (IC50 = 0.06, 2.4, and 3.0 μM, respectively) but not EGFR (IC50 >100 μM).1,2 Through these actions, SU 6668 suppresses tumor growth, blocks angiogenesis in tumors, and induces apoptosis of tumor vasculature and regression of established tumors.3,4,5 It also inhibits metastasis in a mouse orthotopic model of melanoma.6 SU 6668 also inhibits Aurora kinases B and C (IC50 = 35 and 210 nM, respectively) and may target other kinases.7,8

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sun, L., Tran, N., Liang, C., et al. Design, synthesis, and evalutaions of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases. J. Med. Chem. 42(25), 5120-5130 (1999).

    2. Kammasud, N., Boonyarat, C., Sanphanya, K., et al. 5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases. Bioorg. Med. Chem. Lett. 19(3), 745-750 (2009).

    3. Laird, A.D., Vajkoczy, P., Shawver, L.K., et al. SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Res. 60(15), 4152-4160 (2000).

    4. Griffin, R.J., Williams, B.W., Wild, R., et al. Simultaneous inhibition of the receptor kinase activity of vascular endothelial, fibroblast, and platelet-derived growth factors suppresses tumor growth and enhances tumor radiation response. Cancer Res. 62(6), 1702-1706 (2002).

    5. Laird, A.D., Christensen, J.G., Li, G., et al. SU6668 inhibits Flk-1/KDR and PDGFRβ in vivo, resulting in rapid apoptosis of tumor vasculature and tumor regression in mice. The FASEB Journal 16(7), 681-690 (2002).

    6. Gangjee, A., Kurup, S., Ihnat, M.A., et al. Synthesis and biological activity of N4-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents. Bioorg. Med. Chem. 18(10), 3575-3587 (2010).

    7. Godl, K., Gruss, O.J., Eickhoff, J., et al. Proteomic characterization of the angiogenesis inhibitor SU6668 reveals multiple impacts on cellular kinase signaling. Cancer Res. 65(15), 6919-6926 (2005).

    8. Bain, J., Plater, L., Elliot, M., et al. The selectivity of protein kinase inhibitors: A further update. Biochem. J. 408(3), 297-315 (2007).