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.
For research use only. We do not sell to patients.
- CAS No.: 1200127-66-7
- Formula: C22H20N6
- Molecular Weight:368.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Endogenous Metabolite Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | EC50 |
97.7 nM
Compound: 1, GNE-783
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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
|
[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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Molecular Weight 368.43
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)