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Angiogenesis FLT AEE788

AEE788

Catalog No. T2116   CAS 497839-62-0
Synonyms: NVP-AEE 788

AEE788 has been used in trials studying the treatment of Cancer, Glioblastoma Multiforme, and Brain and Central Nervous System Tumors.

AEE788, CAS 497839-62-0
Pack Size Availability Price/USD Quantity
2 mg In stock 74.00
5 mg In stock 134.00
10 mg In stock 232.00
25 mg In stock 480.00
50 mg In stock 734.00
1 mL * 10 mM (in DMSO) In stock 136.00
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Purity 100.00%
Purity 98.00%
Biological Description
Chemical Properties
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Description AEE788 has been used in trials studying the treatment of Cancer, Glioblastoma Multiforme, and Brain and Central Nervous System Tumors.
Targets&IC50 c-Abl ,   c-Fms ,   EGFR ,   FLT1 ,   HER2/ErbB2
Kinase Assay Protein Kinase Assays: The in vitro 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. With the exception of protein kinase C-α, cyclin-dependent kinase 1/cycB and protein kinase A are protamine sulfate (200 μg/mL), histone H1 (100 μg/mL), and the heptapeptide Leu-Arg-Arg-Ala-Ser-Leu-Gly (known as Kemptide Bachem) respectively and are used as peptide substrates. 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 (PDGFR-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 with 1.0% H3PO4 and once with ethanol. Dried membranes are counted after mounting in a Packard TopCount 96-well frame and with the addition of 10 μL/well of Microscint. IC50 values (±SE) are calculated by linear regression analysis of the percentage inhibition and are averages of at least three determinations.
Cell Research
Methylene Blue Cell Proliferation Assay.Cells are seeded at 1.5 × 103 cells/well into 96-well microtiter plates and incubated overnight at 37 °C, 5% v/v CO2 and 80% relative humidity. AEE788 dilutions are added on day 1, with the highest concentration being 10 μM. After incubation of the cell plates for an additional 4 (T24) or 6 (BT-474, SK-BR-3, and NCI-H596) days, cells are fixed with 3.3% v/v glutaraldehyde, washed with water, and stained with 0.05% w/v methylene blue. After washing, the dye is eluted with 3% HCl and the absorbance measured at 665 nm with a SpectraMax 340 spectrophotometer. IC50 values are determined by mathematical curve-fitting and are defined as the drug concentration leading to 50% inhibition of net cell mass increase compared with untreated control cultures. (Only for Reference)
Cell lines: T24, BT-474, SK-BR-3, and NCI-H596 cells
Synonyms NVP-AEE 788
Purity 100.00%
Molecular Weight 440.58
Formula C27H32N6
CAS No. 497839-62-0

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 82 mg/mL (186.1 mM)

Ethanol: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL

Citations

References and Literature
1. Traxler P, et al. Cancer Res, 2004, 64(14), 4931-4941. 2. Park YW, et al. Clin Cancer Res, 2005, 11(5), 1963-1973. 3. Yokoi K, et al. Cancer Res, 2005, 65(9), 3716-3725. 4. Meco D, et al. Transl Oncol, 2010, 3(5), 326-335. 5. Yu C, et al. Clin Cancer Res, 2007, 13(4), 1140-1148.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Apoptosis Compound Library Neuronal Signaling Compound Library Tyrosine kinase inhibitor library Immunology/Inflammation Compound Library Cytokine Inhibitor Library Kinase Inhibitor Library Anti-cancer Clinical Compound Library Angiogenesis related Compound Library JAK STAT Compound Library CNS-Penetrant Compound Library Anti-obesity Compound Library Anti-cancer Active Compound library Anti-cancer Drug library Drug Repurposing Library Target-Focused Phenotypic Screening Library Small Molecule Immuno-Oncology Compound Library Anti-Lung Cancer Compound Library Anti-Breast Cancer Compound Library Anti-Pancreatic Cancer Compound Library Cytoskeletal Signaling Pathway Compound Library

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