GNE-783
GNE-783 is a selective CHK1 inhibitor that enhances the activity of gemcitabine. GNE-783 improves the efficacy of anti-metabolite DNA damage drugs by inactivating S-phase and G2-phase cell cycle checkpoints following DNA damage. GNE-783 selectively enhances the chemical synergy of certain drugs in different tumor types, for example, enhancing the activity of temozolomide only in melanoma cell lines.
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- CAS No.: 1200127-66-7
- Formule: C22H20N6
- Masse moléculaire:368.43
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | EC50 |
97.7 nM
Compound: 1, GNE-783
|
Inhibition of CHK1 in human HT29 cells assessed as phosphorylation of histone H3 after 24 hrs by checkpoint abrogation cellular assay
Inhibition of CHK1 in human HT29 cells assessed as phosphorylation of histone H3 after 24 hrs by checkpoint abrogation cellular assay
|
[PMID: 25988399] |
| HT-29 | GI50 |
>25 μM
Compound: 16, GNE-783
|
Antiproliferative activity against human HT-29 cells assessed as growth inhibition
Antiproliferative activity against human HT-29 cells assessed as growth inhibition
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[PMID: 25453805] |
| HT-29 | IC50 |
0.098 μM
Compound: 16, GNE-783
|
Inhibition of ChK1 in human HT-29 cells assessed as phospho-histone H3 by Isobologram assay
Inhibition of ChK1 in human HT-29 cells assessed as phospho-histone H3 by Isobologram assay
|
[PMID: 25453805] |
Chemical Information
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CAS No. 1200127-66-7
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Masse moléculaire 368.43
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Formule C22H20N6
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SMILES
N#CC1=NC=C2C(C3=CC(C4=CC=C(N5CCN(C)CC5)C=C4)=CN=C3N2)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)