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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- CAS No.: 1304750-47-7
- Formule: C30H38FN3O5S
- Masse moléculaire:571.70
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
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
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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] |
Chemical Information
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CAS No. 1304750-47-7
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Masse moléculaire 571.70
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)