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.
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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: 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.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 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
製品説明
IC50 & Target
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mIDH 6 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-1080 | IC50 |
0.76 nM
Compound: 10; AGI-14100
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Antiproliferative activity against human HT1080 cells transfected with IDH1 R132H mutant
Antiproliferative activity against human HT1080 cells transfected with IDH1 R132H mutant
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[PMID: 29847930] |
| TF-1 | IC50 |
1.75 nM
Compound: 10; AGI-14100
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Antiproliferative activity against human TF1 cells transfected with IDH1 R132H mutant
Antiproliferative activity against human TF1 cells transfected with IDH1 R132H mutant
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[PMID: 29847930] |
| U-87MG ATCC | IC50 |
0.74 nM
Compound: 10; AGI-14100
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Antiproliferative activity against human U87MG cells transfected with IDH1 R132H mutant
Antiproliferative activity against human U87MG cells transfected with IDH1 R132H mutant
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[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.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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)
AGI-14100 関連分類
HY-120181 関連分類
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