1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR

AEE788 (Synonyms: NVP-AEE 788)

Cat. No.: HY-10045 Purity: 99.91%
Handling Instructions

AEE788 is an inhibitor of the EGFR and ErbB2 with IC50 values of 2 and 6 nM, respectively.

For research use only. We do not sell to patients.

AEE788 Chemical Structure

AEE788 Chemical Structure

CAS No. : 497839-62-0

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 158 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 240 In-stock
Estimated Time of Arrival: December 31
50 mg USD 816 In-stock
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Customer Review

    AEE788 purchased from MCE. Usage Cited in: Int J Clin Exp Med. 2016;9(8):15892-15899.

    CNE1 cells are cultured with 3 μM SIS3 for 4 hs, and then washed by cold PBS and followed by the 10 ng/mL TGF-β treatments for 48 hs, respectively.

    AEE788 purchased from MCE. Usage Cited in: Int J Clin Exp Med. 2016;9(8):15892-15899.

    The protein expressions of EGFR are detected by Western blot in CNE1 after 5 nM AEE788 treatment for 4 hs, compared with the control.

    AEE788 purchased from MCE. Usage Cited in: Oncol Rep. 2018 Nov;40(5):2944-2954.

    The EGFR/PI3K/AKT signaling pathway is significantly suppressed in A549 cells treated with AEE788 (0.5 nM, 48 h) following miR-145 upregulation, compared with the miR-145 upregulation group.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    AEE788 is an inhibitor of the EGFR and ErbB2 with IC50 values of 2 and 6 nM, respectively.

    IC50 & Target[1]

    EGFR

    2 nM (IC50)

    ErbB2

    6 nM (IC50)

    In Vitro

    AEE788 inhibits EGFR and VEGF receptor tyrosine kinases in the nM range (IC50:EGFR 2 nm, ErbB2 6 nm, KDR 77 nm, and Flt-1 59 nm). In cells, growth factor-induced EGFR and ErbB2 phosphorylation is also efficiently inhibited (IC50:11 and 220 nm, respectively). AEE788 demonstrates antiproliferative activity against a range of EGFR and ErbB2-overexpressing cell lines (including EGFRvIII-dependent lines) and inhibits the proliferation of epidermal growth factor- and VEGF-stimulated human umbilical vein endothelial cells[1]. Treatment of cutaneous SCC cells with AEE788 leads to dose-dependent inhibition of EGFR and VEGFR-2 phosphorylation, growth inhibition, and induction of apoptosis[2].

    In Vivo

    AEE788 efficiently inhibits growth factor-induced EGFR and ErbB2 phosphorylation in tumors for >72 h. AEE788 also inhibits VEGF-induced angiogenesis in a murine implant model[1]. In mice treated with AEE788, tumor growth is inhibited by 54% at 21 days after the start of treatment compared with control mice[2].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    10 mM in DMSO

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2697 mL 11.3487 mL 22.6974 mL
    5 mM 0.4539 mL 2.2697 mL 4.5395 mL
    10 mM 0.2270 mL 1.1349 mL 2.2697 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    The invitro kinase assays are performed in 96-well plates (30 μL) at ambient temperature for 15–45 min using the recombinant glutathione S-transferase-fused kinase domains (4–100 ng, depending on specific activity). [γ33P]ATP is used as phosphate donor and polyGluTyr-(4:1) peptide as acceptor. Assays are optimized for each kinase using the following ATP concentrations: 1.0 μM (c-Kit, c-Met, c-Fms, c-Raf-1, and RET), 2.0 μM (EGFR, ErbB2, ErbB3, and ErbB4), 5.0 μM (c-Abl), 8.0 μM (Flt-1, Flt-3, Flt-4, Flk, KDR, FGFR-1, and Tek), 10.0 μM (PDGF receptor-β, protein kinase C-α, and cyclin-dependent kinase 1), and 20.0 μM (c-Src and protein kinase A). The reaction is terminated by the addition of 20 μL 125 mM EDTA. Thirty μL (c-Abl, c-Src, insulin-like growth factor-1R, RET-Men2A, and RET-Men2B) or 40 μL (all other kinases) of the reaction mixture is transferred onto Immobilon-polyvinylidene difluoride membrane, presoaked with 0.5% H3PO4 and mounted on a vacuum manifold. Vacuum is then applied and each well rinsed with 200 μL 0.5% H3PO4. Membranes are removed and washed four times. Dried membranes are counted. IC50 are calculated by linear regression analysis of the percentage inhibition and are averages of at least three determinations[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [2]

    AEE788 is dissolved in 90% polyethylene glycol 300 plus 10% 1-methyl-2-pyrrolidinone to a concentration of 6.25 mg/mL. Tumor cells are seeded into 96-well plates in complete medium and allowed to attach for 24 hours. The cultures are re-fed with medium with 2% serum. After 24 hours, cells are treated with different concentrations (0-2 μM) of AEE788 (negative control with DMSO alone) for 72 hours. After a 2-hour incubation in medium containing 0.42 mg/mL MTT, the cells are lysed in 100 μL DMSO. The conversion of MTT to formazan is measured at an absorbance of 570 nm[2]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Mice: AEE788 is diluted in DMSO and diluted in the optimal medium. BALB/c mice bearing s.c. A-431 squamous tumors (3 animals/group) or HC11-NeuT-driven breast tumors (2 animals/group) are dosed orally with 30 mg/kg of AEE788 or vehicle once daily for 5 days. At different time points after the end of compound treatment and before sacrificing the animals the mice are given i.v. 500 μg EGF/kg body weight or 0.2 ml 0.9% w/v NaCl as vehicle control. Five min after EGF administration, the mice are sacrificed, tumors are removed[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    440.58

    Formula

    C₂₇H₃₂N₆

    CAS No.

    497839-62-0

    SMILES

    C[[email protected]](C1=CC=CC=C1)NC2=C(C=C3C(C=C4)=CC=C4CN5CCN(CC)CC5)C(N3)=NC=N2

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
    AEE788
    Cat. No.:
    HY-10045
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    AEE788

    Cat. No.: HY-10045