An inhibitor of EGFR and VEGFR tyrosine kinases
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AEE788

Item No. 18416

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[4-[(4-ethyl-1-piperazinyl)methyl]phenyl]-N-[(1R)-1-phenylethyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
CAS Number
497839-62-0
Synonyms
  • NVP-AEE788
Molecular Formula
C27H32N6
Formula Weight
440.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 25 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/mlEthanol: 5 mg/ml
λmax
236, 327 nm
SMILES
C[C@@H](NC1=C(C=C(C2=CC=C(CN3CCN(CC)CC3)C=C2)N4)C4=NC=N1)C5=CC=CC=C5
InChi Code
InChI=1S/C27H32N6/c1-3-32-13-15-33(16-14-32)18-21-9-11-23(12-10-21)25-17-24-26(28-19-29-27(24)31-25)30-20(2)22-7-5-4-6-8-22/h4-12,17,19-20H,3,13-16,18H2,1-2H3,(H2,28,29,30,31)/t20-/m1/s1
InChi Key
OONFNUWBHFSNBT-HXUWFJFHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $42

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    5 mg

    $132

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    10 mg

    $242

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    25 mg

    $502

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    Product Description

    AEE788 is an inhibitor of both epidermal growth factor (EGF) and vascular endothelial growth factor (VEGF) receptor tyrosine kinase family members.1 It can inhibit EGFR and VEGFR tyrosine kinases with IC50 values of 2, 6, 77, and 59 nM for EGFR, ErbB2, KDR, and FLT1, respectively.1 AEE788 demonstrates antiproliferative activity against a range of EGFR and ErbB2-overexpressing cell lines and can inhibit the proliferation of EGF- and VEGF-stimulated human umbilical vein endothelial cells.1 It also has been shown to have antitumor and anti-angiogenic activity in numerous animal models of cancer.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Traxler, P., Allegrini, P.R., Brandt, R., et al. AEE788: A dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity. Cancer Res. 64(14), 4931-4941 (2004).