Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BI-847325 is a selective dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 45.00 | |
2 mg | In stock | $ 56.00 | |
5 mg | In stock | $ 101.00 | |
10 mg | In stock | $ 177.00 | |
25 mg | In stock | $ 357.00 | |
50 mg | In stock | $ 533.00 | |
100 mg | In stock | $ 769.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 108.00 |
Description | BI-847325 is a selective dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively. |
Targets&IC50 | MEK:4nM, Aurora kinase:15 nM |
In vitro | BI-847325 shows growth-inhibitory effects on BRAF-mutant and vemurafenib-resistant melanoma cells with IC50 ranging from 0.3 nM to 2 μM, and prevents colony formation in six BRAF-mutant melanoma cell lines. BI-847325 also induces apoptosis by reducing Mcl-1 expression. [1] |
In vivo | In mice bearing 1205Lu and 1205LuR xenografts, BI-847325 (75 mg/kg, p.o.) causes significant tumor suppression without significant alteration in the body weights. [1] |
Kinase Assay | Assays are run in the presence of 100 μM ATP using 10 μM of substrate. 30 μL PROTEIN-MIX in 25% DMSO and incubated for 15 min at room temperature. 10 μL PEPTIDE-MIX is added, the mixture is incubated for 60 min at RT and stopped by adding 180 μL 6.4% TCA (final concentration: 5%). Incorporated phosphate is measured in a scintillation counter and IC50 values are calculated using a sigmoidal curve analysis program with variable hill slope[1]. |
Cell Research | Cells are plated at a density of 2.5 × 103 cells per 100 μL and left to grow overnight before being treated with increasing concentrations of BI-847325 for 72 hours. The metabolic activity is determined using Alamar blue reagent as per the manufacturer's protocol.(Only for Reference) |
Molecular Weight | 464.56 |
Formula | C29H28N4O2 |
CAS No. | 1207293-36-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 18 mg/mL (38.7 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 1 mg/mL (2.15 mM)
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
BI-847325 1207293-36-4 Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic MAPK MEK Aurora Kinase BI847325 inhibit MAPKK MAP2K Inhibitor Mitogen-activated protein kinase kinase BI 847325 inhibitor