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BI-847325

Catalog No. T6785   CAS 1207293-36-4

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.

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BI-847325 Chemical Structure
BI-847325, CAS 1207293-36-4
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
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Purity: 97.54%
Purity: 97.13%
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Biological Description
Chemical Properties
Storage & Solubility Information
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 kinases (AK):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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 18 mg/mL (38.7 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 1 mg/mL (2.15 mM)

TargetMolReferences and Literature

1. Phadke MS, et al. Mol Cancer Ther. 2015, 14(6), 1354-1364.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Drug Repurposing Compound Library Anti-Liver Cancer Compound Library Glutamine Metabolism Compound Library Anti-Pancreatic Cancer Compound Library Kinase Inhibitor Library Anti-Prostate Cancer Compound Library

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Keywords

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

 

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