AEE788
Based on 3 publication(s) in Google Scholar
AEE788 is an orally active inhibitor targeting EGFR and ErbB2 with IC50 values of 2 and 6 nM, respectively[1][2][3].
For research use only. We do not sell to patients.
- Purity: 98.39%
- CAS No.: 497839-62-0
- Formula: C27H32N6
- Molecular Weight:440.58
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) AEE788
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Customer Validation & Images
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All EGFR Isoforms
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Biological Activity
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EGFR 2 nM (IC50) |
ErbB2 6 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| D283 Med | IC50 |
3.8 μM
Compound: AEE788
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Antitumor activity against human D283 Med cells assessed as inhibition of cell proliferation
Antitumor activity against human D283 Med cells assessed as inhibition of cell proliferation
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[PMID: 33636537] |
| Daoy | IC50 |
1.7 μM
Compound: AEE788
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Antitumor activity against human Daoy cells assessed as inhibition of cell proliferation
Antitumor activity against human Daoy cells assessed as inhibition of cell proliferation
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[PMID: 33636537] |
| Huh-7 | CC50 |
27.83 μM
Compound: GNF-Pf-5343
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NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
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[PMID: 18579783] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 497839-62-0
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Appearance Solid
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Molecular Weight 440.58
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Formula C27H32N6
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Color White to off-white
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SMILES
C[C@H](C1=CC=CC=C1)NC2=C(C=C3C(C=C4)=CC=C4CN5CCN(CC)CC5)C(N3)=NC=N2
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Synonyms
NVP-AEE 788
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Oncol Rep
MicroRNA‑145 inhibits migration and induces apoptosis in human non‑small cell lung cancer cells through regulation of the EGFR/PI3K/AKT signaling pathway. [Abstract]2018 Nov;40(5):2944-2954. PMID: 30226581
AEE788 purchased from MedChemExpress. Usage Cited in: Oncol Rep. 2018 Nov;40(5):2944-2954. [Abstract]
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.
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AEE788 purchased from MedChemExpress. 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.
Solvent & Solubility
DMSO : 50 mg/mL (113.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.67 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Traxler P, 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. 2004 Jul 15;64(14):4931-4941. [Content Brief]
[2]. Park et al. AEE788, a dual tyrosine kinase receptor inhibitor, induces endothelial cell apoptosis in human cutaneous squamous cell carcinoma xenografts in nude mice. Clin Cancer Res. 2005 Mar 1;11(5):1963-1973. [Content Brief]
[3]. Goudar RK, et al. Combination therapy of inhibitors of epidermal growth factor receptor/vascular endothelial growth factor receptor 2 (AEE788) and the mammalian target of rapamycin (RAD001) offers improved glioblastoma tumor growth inhibition. Mol Cancer Ther. 2005 Jan;4(1):101-12. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2697 mL | 11.3487 mL | 22.6974 mL | 56.7434 mL |
| 5 mM | 0.4539 mL | 2.2697 mL | 4.5395 mL | 11.3487 mL | |
| 10 mM | 0.2270 mL | 1.1349 mL | 2.2697 mL | 5.6743 mL | |
| 15 mM | 0.1513 mL | 0.7566 mL | 1.5132 mL | 3.7829 mL | |
| 20 mM | 0.1135 mL | 0.5674 mL | 1.1349 mL | 2.8372 mL | |
| 25 mM | 0.0908 mL | 0.4539 mL | 0.9079 mL | 2.2697 mL | |
| 30 mM | 0.0757 mL | 0.3783 mL | 0.7566 mL | 1.8914 mL | |
| 40 mM | 0.0567 mL | 0.2837 mL | 0.5674 mL | 1.4186 mL | |
| 50 mM | 0.0454 mL | 0.2270 mL | 0.4539 mL | 1.1349 mL | |
| 60 mM | 0.0378 mL | 0.1891 mL | 0.3783 mL | 0.9457 mL | |
| 80 mM | 0.0284 mL | 0.1419 mL | 0.2837 mL | 0.7093 mL | |
| 100 mM | 0.0227 mL | 0.1135 mL | 0.2270 mL | 0.5674 mL |
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