AGI-14100
AGI-14100 is a metabolically stable and orally available mIDH1 inhibitor (IC50=6 nM). The pharmacochemical optimization of AGI-14100 is aimed at eliminating hPXR activation, resulting in the final drug candidate AG-120. AG-120 can be used in the study of cancers carrying IDH1 mutations. The discovery and development of AGI-14100 can be used for further studies of mutant isocitrate dehydrogenase 1 (mIDH1) inhibitors.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 1448346-43-7
- 分子式: C29H22ClF4N5O3
- 分子量:599.96
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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mIDH 6 nM (IC50) |
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HT-1080 | IC50 |
0.76 nM
Compound: 10; AGI-14100
|
Antiproliferative activity against human HT1080 cells transfected with IDH1 R132H mutant
Antiproliferative activity against human HT1080 cells transfected with IDH1 R132H mutant
|
[PMID: 29847930] |
| TF-1 | IC50 |
1.75 nM
Compound: 10; AGI-14100
|
Antiproliferative activity against human TF1 cells transfected with IDH1 R132H mutant
Antiproliferative activity against human TF1 cells transfected with IDH1 R132H mutant
|
[PMID: 29847930] |
| U-87MG ATCC | IC50 |
0.74 nM
Compound: 10; AGI-14100
|
Antiproliferative activity against human U87MG cells transfected with IDH1 R132H mutant
Antiproliferative activity against human U87MG cells transfected with IDH1 R132H mutant
|
[PMID: 29847930] |
化学情報
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CAS 番号 1448346-43-7
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分子量 599.96
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分子式 C29H22ClF4N5O3
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SMILES
O=C([C@@H](N1C2=NC=CC(C#N)=C2)CCC1=O)N([C@@H](C3=CC=CC=C3Cl)C(NC4CC(C4)(F)F)=O)C5=CC(F)=CC(F)=C5
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輸送条件
Room temperature in continental US; may vary elsewhere.
-
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)
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