BRD2879
BRD2879 is a potent IDH1-R132H inhibitor with IC50 values of 0.05, 2.5, >20, >20 µM for IDH1-R132H, IDH1-R132C, IDH1-WT, IDH2-R140Q, respectively. BRD2879 reduces (R)-2-hydroxyglutarate (R-2HG) levels.
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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: 1304750-47-7
- 分子式: C30H38FN3O5S
- 分子量:571.70
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
R132H IDH1 0.05 μM (IC50) |
R132C IDH1 2.5 μM (IC50) |
IDH1 wt >20 μM (IC50) |
IDH2-R140Q >20 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
>20 μM
Compound: BRD2879
|
Inhibition of human C-terminal FLAG-tagged IDH1-R140Q mutant (1 to 452 residues) expressed in baculovirus infeceted sf9 cells assessed as inhibition of ketoreductase activity preincubated for 10 mins followed by addition of NADPH and alpha-KG as substrate
Inhibition of human C-terminal FLAG-tagged IDH1-R140Q mutant (1 to 452 residues) expressed in baculovirus infeceted sf9 cells assessed as inhibition of ketoreductase activity preincubated for 10 mins followed by addition of NADPH and alpha-KG as substrate
|
[PMID: 27774134] |
化学情報
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CAS 番号 1304750-47-7
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分子量 571.70
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分子式 C30H38FN3O5S
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SMILES
O=S1(C2=CC=C(C#CC3=CC(F)=CC=C3)C=C2O[C@H]([C@@H](CN1[C@@H](C)CO)C)CN(C)C(NC4CCCCC4)=O)=O
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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)