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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 1304750-47-7
- Fòrmula: C30H38FN3O5S
- Peso molecular:571.70
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
Actividad biológica
Descripciòn
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
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[PMID: 27774134] |
Chemical Information
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No. CAS 1304750-47-7
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Peso molecular 571.70
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocolo
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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.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)