Osu03012

SKU: orb1305446

Description

Osu03012

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 742112-33-0
• MW: 460.45
• Purity: 98.47%
• Formula: C₂₆H₁₉F₃N₄O
• SMILES: NCC(=O)Nc1ccc(cc1)-n1nc(cc1-c1ccc2c(ccc3ccccc23)c1)C(F)(F)F
• Target: PDK,Autophagy
• Solubility: DMSO:120 mg/mL (260.61 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.34 mM)

Bioactivity

• Target IC50:
  PDK1:5 μM
• In Vivo:
  At concentrations of 3-5 μM, OSU-03012 can completely inhibit the growth of various tumor cells. In thyroid cancer cells (NPA, WRO, and ARO cells), OSU-03012 acts as an ATP-competitive inhibitor, inhibiting cell proliferation and migration, and inducing apoptosis by suppressing PAK activity and AKT phosphorylation. In hepatocellular carcinoma cell lines (Huh7, Hep3B, and HepG2 cells), OSU-03012 (IC50<1 μM) inhibits cell growth, notably inducing autophagy in Huh7 cells. Additionally, in glioblastoma and PC-3 cells, OSU-03012 promotes apoptosis.
• In Vitro:
  In the MDA-MB-435/LCC6 xenograft model, OSU-03012 significantly reduced the expression of EGFR protein in tumors while also inhibiting the binding of YB-1 to the EGFR promoter. In Huh7 xenografts, OSU-03012 (200 mg/kg) effectively inhibited tumor cell growth. Similarly, oral administration of OSU-03012 in the HMS-97 neurofibroma xenograft model suppressed cell growth.
• Cell Research:
  The effect of OSU-03012 on PC-3 cell viability is assessed by using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide assay in six replicates. Cells are grown in 10% FBS- supplemented RPMI 1640 in 96-well, flat-bottomed plates for 24 hours. They are exposed to various concentrations of OSU-03012 (0-10 μM) dissolved in DMSO (final concentration ≤0.1%) in 1% serum-containing RPMI 1640 for different time intervals (~72 hours). Controls receive DMSO vehicle at a concentration equal to that in OSU-03012-treated cells. The medium is removed and replaced by 200 μL of 0.5 mg/mL 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide in 10% FBS-containing RPMI 1640. The cells are incubated in the CO2 incubator at 37 °C for 2 hours. Supernatants are removed from the wells, and the reduced 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide dye is solubilized in 200 μL DMSO per well. Absorbance at 570 nm is determined by using a plate reader.(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

AR12, AR-12, AR 12, Osu 03012, Osu03012, Osu-03012, PDK1

Compound Identifiers

PubChem CID

10027278