Chemical Property of PDK1 inhibitor AR-12
Chemical Property:
- Vapor Pressure:0mmHg at 25°C
- Refractive Index:1.649
- Boiling Point:683.017 °C at 760 mmHg
- Flash Point:366.876 °C
- PSA：72.94000
- Density:1.369 g/cm3
- LogP:6.53500
- Solubility.:≥23 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
- XLogP3:5.2
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:6
- Rotatable Bond Count:4
- Exact Mass:460.15109573
- Heavy Atom Count:34
- Complexity:711
- Purity/Quality:
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99%, *data from raw suppliers
OSU03012 *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:C1=CC=C2C(=C1)C=CC3=C2C=CC(=C3)C4=CC(=NN4C5=CC=C(C=C5)NC(=O)CN)C(F)(F)F
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Description
Cyclooxygenase-2 (COX-2) appears to play a significant role in the development and progression of cancer and COX-2 inhibitors such as celecoxib exhibit anti-cancer activity. OSU03012 is an analog of celecoxib that exhibits anti-cancer activity in a COX-2-independent manner via inhibition of the phosphatidyl inositol-3-kinase/Akt pathway. It has an IC50 value of 5 μM for inhibition of 3-phosphoinositide-dependent kinase-1, and therefore Akt activation, with no measurable COX-2 inhibition up to 50 μM. OSU03012 is a potent inhibitor of tumor cell growth with an average inhibitory concentration of 1.1 μM across a panel of 60 cancer cell lines. It does not inhibit signal transduction through the mitogen-activated protein kinase (MAPK) pathway. OSU03012 induces apoptosis of chronic lymphocytic leukemia cells independent of bcl-2 overexpression using both caspase-dependent and independent pathways.
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Uses
OSU 03012 is a PDK1 inhibitor and inducer of caspase and p53-independent apoptosis, also used in the development of anticancer agents by modification of novel immunosuppressant FTY720 and PDK1 inhibitor OSU-03012, compound for treating Alzheimers diseases.
