MBQ-167

SKU: orb1308056

Description

MBQ-167 is a potent dual inhibitor targeting Rac and Cdc42 GTPases, exhibiting IC50 values of 103 nM and 78 nM, respectively, in cellular assays. This compound is a valuable research tool for investigating cytoskeletal dynamics, cell migration, and invasion in cancer research, with demonstrated utility in both in vitro and in vivo experimental models.

Research Area

Cell Biology, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 2097938-73-1
• MW: 338.41
• Purity: 99.52% (May vary between batches)
• Formula: C₂₂H₁₈N₄
• SMILES: CCn1c2ccccc2c2cc(ccc12)-n1nncc1-c1ccccc1
• Target: CDK,Ras
• Solubility: H2O:< 0.1 mg/mL (insoluble);DMSO:155 mg/mL (458.02 mM)

Bioactivity

• Target IC50:
  Ras1/2/3:103 nM|CDC42:78 nM
• In Vivo:
  Mice treated with MBQ-167 exhibited comparable doubling times for the treatments (10 and 11 days), and demonstrated a statistically significant decrease in tumor growth. Upon sacrifice, a dosage of 1.0 mg/kg body weight (BW) with MBQ-167 led to an approximate 80% reduction in tumor size, while a higher dose of 10 mg/kg BW achieved an approximate 95% reduction. In comparison, EHop-016 at a 10 mg/kg BW dosage resulted in about a 40% reduction in tumor growth, making MBQ-167 ten times more effective than EHop-016.
• In Vitro:
  MBQ-167 causes this phenotype in multiple mesenchymal cancer cell types including GFP-HER2-BM, MDA-MB-468, and Hs578t human breast cancer cells, as well as Mia-PaCa-2 pancreatic cancer cells, SKOV3 ovarian cancer cells, AGS and NCI-N87 gastric cancer cells, and SH-SY5Y neuroblastoma cells. MBQ-167 (≥100 nM) causes a loss of polarity in metastatic breast cancer cells. MBQ-167(500 nM; 24 h)treatment, results in ~95% cell rounding and detachment from the substratum in metastatic MDA-MB-231 cells. At earlier times (6h), MBQ-167(250 or 500 nM)treatment, induce an inhibition in Rac activity in the attached cell population, while the detached population demonstrates a ~40-50% inhibition. The attached population of MDA-MB-231 cells demonstrate a ~25% decrease in Rac activation while the detached cells are more responsive with a ~75% decrease following treatment with 250 nM MBQ-167 for 24 h .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ras 1/2/3, Ras, Cyclin dependent kinase, CDK, Cdc42, inhibit, Inhibitor, MBQ 167, MBQ167, MBQ-167

Compound Identifiers

PubChem CID

129896932