| Name | BI-847325 |
| 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. |
| 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) |
| 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]. |
| 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] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 50 mg/mL (107.63 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 1 mg/mL (2.15 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.15 mM), Sonication is recommended.
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| Keywords | Mitogen-activated protein kinase kinase | MEK2 | MEK1 | MEK | MAPKK | MAP2K | Inhibitor | inhibit | BI-847325 | BI847325 | BI 847325 | AuroraKinase | Aurora Kinase | Aurora C (Human) | Aurora B (Xenopus laevis) | Aurora A (Human) | Apoptosis |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sodium Molybdate | Sildenafil citrate |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
