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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1200127-66-7
- 分子式: C22H20N6
- 分子量:368.43
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Endogenous Metabolite アイソフォーム固有の製品をすべて表示
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生物活性
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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
|
[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] |
化学情報
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CAS 番号 1200127-66-7
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分子量 368.43
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)