TAK-632

SKU: orb1307266

Description

TAK-632

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 1228591-30-7
• MW: 554.52
• Purity: 98.50%
• Formula: C₂₇H₁₈F₄N₄O₃S
• SMILES: Fc1ccc(Oc2ccc3nc(NC(=O)C4CC4)sc3c2C#N)cc1NC(=O)Cc1cccc(c1)C(F)(F)F
• Target: Aurora Kinase,Raf,PDGFR,FGFR
• Solubility: Ethanol:2 mg/mL (3.61 mM);DMSO:93 mg/mL (167.71 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+90% Corn Oil:3.3 mg/mL (5.95 mM)

Bioactivity

• Target IC50:
  Tie2:740 nM|p38α:600 nM|C-Raf:1.4 nM|CDK1:790 nM|IKKβ:3700 nM|B-Raf:8.3 nM|MEK1:3700 nM|GSK-3β:500 nM|CDK2:580 nM|PDGFRβ:120 nM|PDGFRα:610 nM|FGFR3:280 nM|Aurora B:66 nM
• In Vivo:
  TAK-632 effectively inhibits cell proliferation in A375 (GI50=66 nM) and HMVII cell lines (GI50=200 nM). Specifically, in the melanoma A375 cell line (BRAFV600E), TAK-632 suppresses MEK phosphorylation (IC50=2 nM) and ERK phosphorylation (IC50=16 nM). Additionally, in the human melanoma HMVII cell line (NRASQ61K/BRAFG469V), TAK-632 inhibits pMEK (IC50=49 nM) and pERK (IC50=50 nM).
• In Vitro:
  In an SK-MEL-2 xenograft mouse model bearing NRAS-mutant melanoma, oral administration of TAK-632 (at doses of 60 or 120 mg/kg) inhibits the MAPK signaling pathway, thereby suppressing tumor growth.
• Cell Research:
  The cells are proliferated in appropriate medium (vender recommended) supplemented with 10% heat-inactivated fetal bovine serum (FBS) and antibiotics, in tissue culture dishes placed in a humidified incubator maintained at 37°C in an atmosphere of 5% CO2 and 95% air. The anti-proliferative activity of compound is determined by treating cell lines with the compound for 3 days, followed by measurement of viable cell number in the Cell Titer-Glo assay. The cells are seeded in a 96-multiwell plate at 1500 to 4000 cells per well in medium containing FBS and cells allowed to sit down overnight. After 18–20 h, compounds at various concentrations by serial dilution are added to the cells and were cultured for 3 days in chamber. After the treatment culture, cellular proliferation is determined by a Cell Titer-Glo Luminescent Cell Viability Assay. In brief, 100 bL/well of Cell Titer-Glo Substrate solution is added to each well and the cells were cultured for an additional 10 minutes (approximately). The chemi-luminescence value is measured using a Luminescence Counter 1420 ARVO MX Light. Concentration response curves are generated by calculating the decrease in chemi-luminescence values in compound-treated samples relative to the vehicle (DMSO) treated controls. (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.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TAK632, TAK-632, TAK 632, Raf, Raf kinases, B-Raf, Aurora B, AuroraKinase, Aurora Kinase, C-Raf, FGFR3, PDGFRβ, inhibit, Inhibitor

Compound Identifiers

PubChem CID

46209401