BI-847325

SKU: orb1300468

Description

BI-847325 is a potent small molecule that selectively inhibits both MEK2 and Aurora Kinase C with IC50 values of 4 nM and 15 nM, respectively. It is utilized in cancer research to study pathway signaling and has demonstrated antitumor activity in both cellular assays and in vivo xenograft models.

Research Area

Cell Biology, Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 1207293-36-4
• MW: 464.56
• Purity: 97.13%
• Formula: C₂₉H₂₈N₄O₂
• SMILES: CCNC(=O)C#Cc1ccc2\C(=C(\Nc3ccc(CN(C)C)cc3)c3ccccc3)C(=O)Nc2c1
• Target: MEK,Aurora Kinase,Apoptosis
• Solubility: Ethanol:1 mg/mL (2.15 mM);DMSO:18 mg/mL (38.75 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.15 mM)

Bioactivity

• Target IC50:
  Aurora kinase:15 nM|MEK: nM
• 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.
• 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.
• Cell Research:
  Cells are plated at a density of 2.5 × 10^3 cells per 100 μL and left to grow overnight before being treated with increasing concentration of BI-847325 for 72 hours the metabolic activity is determined using Alamar blue reagent as pe the manufacturer's protocol.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Apoptosis, AuroraKinase, Aurora Kinase, Aurora B (Xenopus laevis), Aurora C (Human), Aurora A (Human), BI847325, BI-847325, BI 847325, MAPKK, MAP2K, MEK, MEK1, MEK2, Inhibitor, Mitogen-activated protein kinase kinase, inhibit

Compound Identifiers

PubChem CID

135567102