| Field | Specification |
|---|---|
| Alternative names | AR-12; PDK1 inhibitor AR-12 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C26H19F3N4O |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
OSU-03012, also known as AR-12 and PDK1 inhibitor AR-12, is a blood-brain-permeable inhibitor of PDK-1, with an IC50 of 5 μM[1][3]. It is supplied as a white to off-white solid (C26H19F3N4O, MW 460.45) at 99.80% purity.
Physical & Chemical Properties
| CAS Number | 742112-33-0 |
|---|---|
| Molecular Formula | C26H19F3N4O |
| Molecular Weight | 460.45 g/mol |
| Purity | 99.80% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=C(CN)NC1=CC=C(C=C1)N2N=C(C=C2C3=CC=C4C5=CC=CC=C5C=CC4=C3)C(F)(F)F |
| Signaling Pathway | PI3K/Akt/mTOR; Autophagy |
| Solubility | In Vitro: DMSO: ≥ 100 mg/mL (217.18 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) * "≥" means soluble, but saturation unknown. |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 5 μM (PDK-1)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | ≥ 100 mg/mL (217.18 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (5.43 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | 2.5 mg/mL (5.43 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 2.5 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (5.43 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
OSU-03012 reduces PC-3 cell viability, with an IC50 value of 5 μM. PC-3 cell proliferation in 10% FBS-supplemented medium is also assessed under OSU-03012 treatment. In 1% FBS-containing medium, OSU-03012 induces apoptotic death of PC-3 cells in a dose-dependent manner, shown by DNA fragmentation and PARP cleavage. OSU-03012 suppresses PC-3 cell proliferation at sub-μM concentrations, consistent with the result in 1% serum[1].
In Vivo
Two MDA-MB-435/LCC6/Her-2 tumors develop in every SCID/Rag2 mouse, and the mice are then assigned to a vehicle control group or an OSU-03012 (200 mg/kg) treatment group, the latter dosed orally for 3 days. EGFR protein expression in the tumors falls remarkably, by ~48%, with OSU-03012, relative to levels in tumors from mice that receive the vehicle control. Binding of Y-box binding protein-1 (YB-1) to the EGFR promoter at the 1b and 2a sites is also prevented by OSU-03012[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Cell Assay[1]
Culture PC-3 (p53-/-) human androgen-nonresponsive prostate cancer cells at 37°C in a humidified 5% CO2 incubator, in RPMI 1640 containing 10% fetal bovine serum (FBS). Test Celecoxib and its derivatives (e.g., OSU-03012) at 2.5 μM, 5 μM, 7.5 μM and 10 μM for effects on PC-3 cell viability by MTT assay in six replicates. Grow cells in 96-well, flat-bottomed plates in 10% FBS-supplemented RPMI 1640 for 24 h, then expose them to Celecoxib derivatives (e.g., OSU-03012) at various concentrations, dissolved in DMSO (final concentration ≤0.1%), in 1% serum-containing RPMI 1640 for different time intervals. Give controls DMSO vehicle at a concentration equal to that in drug-treated cells. Remove the medium, replace it with 200 μL of 0.5 mg/mL MTT in 10% FBS-containing RPMI 1640, and incubate cells at 37°C for 2 h in the CO2 incubator. Remove supernatants from the wells and solubilize the reduced MTT dye in 200 μL/well DMSO. Measure absorbance at 570 nm on a plate reader[1].
Animal Administration[2]
Mice[2] Inject SCID/Rag2m mice (6-8 weeks old, female) subcutaneously with 1×107 MDA-MB-435/LCC6 cells stably transfected with HER-2/neu. Inoculate each mouse on the right and left sides of the lower back with the cells; inject a total of eight mice, each harboring two tumors. After 6 weeks, randomly assign the mice to a vehicle group (0.5% methyl cellulose/0.1% Tween 80) or an OSU-03012 at 200 mg/kg/day group. Give mice either the vehicle or OSU-03012 by oral gavage, daily for 3 days. On the fourth day, end the study, sacrifice the mice, and collect the tumors for chromatin immunoprecipitation (ChIP) and protein isolations.
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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