BINIMETINIB

Binimetinib is a MEK1/2 inhibitor blocking MAPK signaling, used for BRAF‑mutant melanoma. Side effects include retinal changes, CPK elevation, diarrhea, rash, and cardiomyopathy.

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Product Description


Mechanism of Action

BINIMETINIB (ID 30034) displays a high‑dimensional biochemical interaction profile, integrating catalytic‑domain modulation, multi‑axis signalling interference, mitochondrial‑network recalibration, ion‑flux redistribution, membrane‑potential rebalancing, cytoskeletal remodelling, redox‑equilibrium restructuring and transcription‑factor pathway reprogramming. Its molecular topology supports interaction with catalytic residues, allosteric microdomains, transmembrane helices, nucleotide‑binding pockets, redox‑buffer centres and polymeric scaffolding complexes, enabling wide‑band influence across metabolic, genomic, structural and electrophysiological layers.

At the signalling level, BINIMETINIB may reconfigure phosphorylation landscapes spanning ERK/MAPK/JNK/p38 and PI3K–AKT axes, modulate G‑protein coupling states, reorganise Ca²⁺ microdomain geometry, adjust IP₃/DAG cascade topology, and recalibrate cAMP–PKA amplitude distributions. Mitochondrial effects can include ETC‑complex rebalancing, ATP/ADP flux modulation, ROS‑threshold displacement, membrane‑potential polarity shifts and bidirectional stress‑signal integration between ER and mitochondrial compartments.

Advanced Research Applications

  • Kinome‑scale catalytic‑cascade interference mapping
  • High‑resolution docking & conformational‑transition simulations
  • UPR/ER‑stress, mitophagy & autophagic‑flux network analysis
  • Full multi‑omics integration (RNA‑seq, proteomics, phosphoproteomics, metabolomics)
  • Cytoskeletal mechanics & polymer‑turnover/force‑distribution modelling
  • Cell‑fate pathway simulations (apoptosis, necroptosis, ferroptosis, parthanatos)
  • AI‑driven SAR/QSAR pipelines for compound‑performance prediction

Toxicodynamics & Hazard Spectrum

  • Rapid ROS escalation & antioxidant‑buffer saturation
  • Mitochondrial fragmentation or ETC‑axis suppression
  • Severe Na⁺/K⁺/Ca²⁺ ionic‑flux destabilisation
  • Cytoskeletal depolymerisation & membrane‑integrity loss
  • Hyperactivation of NF‑κB, STAT & IRF inflammatory regulators
  • Induction of multi‑axis programmed‑cell‑death pathways
  • Epigenetic drift including methylation/acetylation imbalance

For expert laboratory research only — not intended for biological or therapeutic exposure.

Datasheet


Molecular Formula

C17H15BrF2N4O3

Molecular Weight

441.2 g/mol

CAS Number

606143-89-9

Storage Condition

Store in a cool, dry place. Keep container tightly closed. Protect from moisture and light.

Solubility

Solubility depends on solvent and conditions (e.g., pH). Please contact us for solvent-specific guidance.

Purity

Purity information is available upon request (COA).

Synonym

Binimetinib; 606143-89-9; MEK162; Mektovi; ARRY-162

IUPAC/Chemical Name

6-(4-bromo-2-fluoroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide

InChl Key

ACWZRVQXLIRSDF-UHFFFAOYSA-N

InChl Code

InChI=1S/C17H15BrF2N4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26)

References

https://pubchem.ncbi.nlm.nih.gov/compound/10288191;

3D Conformer.

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