Cat. No.: HY-10547

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OSU-03012

(Synonyms: AR-12; PDK1 inhibitor AR-12)

8 Cited Publications

Customer Review

Based on 8 publication(s) in Google Scholar

OSU-03012 (AR-12; PDK1 inhibitor AR-12) is a blood-brain permeable PDK-1 inhibitor with an IC₅₀ of 5 μM.

For research use only. We do not sell to patients.

Purity: 99.80%
CAS No.: 742112-33-0
Formula: C₂₆H₁₉F₃N₄O
Molecular Weight:460.45

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

OSU-03012 Chemical Structure

CAS No.: 742112-33-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (8)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

OSU-03012 (AR-12; PDK1 inhibitor AR-12) is a blood-brain permeable PDK-1 inhibitor with an IC₅₀ of 5 μM^[1]^[3].

IC₅₀ & Target

IC50: 5 μM (PDK-1)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	IC₅₀	2.9 μM Compound: OSU-0312	Cytotoxicity against human 786-0 cells measured after 72 hrs by MTT assay Cytotoxicity against human 786-0 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
A673	IC₅₀	2.1 μM Compound: OSU-0312	Cytotoxicity against human A673 cells measured after 72 hrs by MTT assay Cytotoxicity against human A673 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
CAKI-1	IC₅₀	5 μM Compound: OSU-0312	Cytotoxicity against human CAKI-1 cells measured after 72 hrs by MTT assay Cytotoxicity against human CAKI-1 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
HCT-116	IC₅₀	2.7 μM Compound: OSU-0312	Cytotoxicity against human HCT-116 cells measured after 72 hrs by MTT assay Cytotoxicity against human HCT-116 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
HT-29	IC₅₀	3.6 μg/mL Compound: 23	Antiproliferative activity against human HT-29 cells after 24 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 24 hrs by MTT assay	[PMID: 22750009]
Huh-7	CC₅₀	>10 μM Compound: 63; OSU-03012, AR-12	Cytotoxicity against human Huh-7 cells Cytotoxicity against human Huh-7 cells	[PMID: 33539089]
IGROV-1	IC₅₀	3.7 μM Compound: OSU-0312	Cytotoxicity against human IGROV-1 cells measured after 72 hrs by MTT assay Cytotoxicity against human IGROV-1 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
MCF7	IC₅₀	2.8 μM Compound: OSU-0312	Cytotoxicity against human MCF7 cells measured after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
NCI-H69	IC₅₀	1.8 μM Compound: OSU-0312	Cytotoxicity against human NCI-H69 cells measured after 72 hrs by MTT assay Cytotoxicity against human NCI-H69 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
NCI-H82	IC₅₀	4 μM Compound: OSU-0312	Cytotoxicity against human NCI-H82 cells measured after 72 hrs by MTT assay Cytotoxicity against human NCI-H82 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
PC-3	IC₅₀	6.5 μM Compound: OSU-0312	Cytotoxicity against human PC-3 cells measured after 72 hrs by MTT assay Cytotoxicity against human PC-3 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
RAW264.7	CC₅₀	7.7 μM Compound: AR12	Cytotoxicity against mouse RAW264.7 cells assessed as reduction in number of cells by DAPI staining based high-content image analysis Cytotoxicity against mouse RAW264.7 cells assessed as reduction in number of cells by DAPI staining based high-content image analysis	[PMID: 36439974]
RAW264.7	IC₅₀	0.2 μM Compound: AR-12, OSU-03012	Antimicrobial activity against Salmonella enterica serovar Typhimurium ATCC 14028 infected in mouse RAW264.7 cells assessed as inhibition of intracellular bacterial growth after 8 hrs Antimicrobial activity against Salmonella enterica serovar Typhimurium ATCC 14028 infected in mouse RAW264.7 cells assessed as inhibition of intracellular bacterial growth after 8 hrs	[PMID: 19805568]
RAW264.7	IC₅₀	10 μM Compound: AR-12, OSU-03012	Cytotoxicity against mouse RAW264.7 cells assessed as cell viability after 24 hrs by MTT assay Cytotoxicity against mouse RAW264.7 cells assessed as cell viability after 24 hrs by MTT assay	[PMID: 19805568]
Rec1	IC₅₀	3.8 μM Compound: OSU-0312	Cytotoxicity against human REC1 cells measured after 72 hrs by MTT assay Cytotoxicity against human REC1 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
SK-N-MC	IC₅₀	6 μM Compound: OSU-0312	Cytotoxicity against human SK-N-MC cells measured after 72 hrs by MTT assay Cytotoxicity against human SK-N-MC cells measured after 72 hrs by MTT assay	[PMID: 34624821]
TC-32	IC₅₀	2 μM Compound: OSU-0312	Cytotoxicity against human TC-32 cells measured after 72 hrs by MTT assay Cytotoxicity against human TC-32 cells measured after 72 hrs by MTT assay	[PMID: 34624821]

In Vitro

OSU-03012 inhibits PC-3 cells viability with IC₅₀ values of 5 μM. The effects of OSU-03012 on PC-3 cell proliferation in 10% FBS-supplemented medium are also examined. OSU-03012 induces apoptotic death in PC-3 cells in 1% FBS-containing medium in a dose-dependent manner, as demonstrated by DNA fragmentation and PARP cleavage. OSU-03012 is effective in suppressing PC-3 cell proliferation at sub-μM, consistent with that noted in 1% serum^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

All of the SCID/Rag2 mice develop two MDA-MB-435/LCC6/Her-2 tumors and are assigned to either the vehicle control or OSU-03012 (200 mg/kg) treatment group, which is given orally for 3 days. OSU-03012 remarkably decreases EGFR protein expression in the tumors by ~48% compared with expression levels found in the tumors taken from mice that receive the vehicle control. OSU-03012 also prevents Y-box binding protein-1 (YB-1) from binding to the EGFR promoter at the 1b and 2a sites^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 742112-33-0
Appearance Solid
Molecular Weight 460.45
Formula C₂₆H₁₉F₃N₄O
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
Synonyms

AR-12; PDK1 inhibitor AR-12
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (8)

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Journal Impact Factor

Science

Neuronal FAM171A2 mediates α-synuclein fibril uptake and drives Parkinson's disease. [Abstract]

2025 Feb 21;387(6736):892-900. PMID: 39977508
Autophagy

Stimulating the autophagic-lysosomal axis enhances host defense against fungal infection in a zebrafish model of invasive Aspergillosis. [Abstract]

2023 Jan;19(1):324-337. PMID: 35775203
J Adv Res

Low temperatures enhance PM2.5-mediated mitochondrial dysfunction in the pig lung-intestinal axis, causing damage to the gut. [Abstract]

2026 May 3:S2090-1232(26)00380-2. PMID: 42086185
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Antimicrob Agents Chemother

AR-12 Exhibits Direct and Host-Targeted Antibacterial Activity toward Mycobacterium abscessus. [Abstract]

2020 Jul 22;64(8):e00236-20. PMID: 32482678
J Virol

Microfilaments and microtubules alternately coordinate the multi-step endosomal trafficking of Classical Swine Fever Virus. [Abstract]

2021 Feb 24;95(10):e02436-20. PMID: 33627389
Biomed Pharmacother

Drug target proteome profiling identifies HES1-driven mitotic catastrophe in ovarian serous carcinoma. [Abstract]

2025 Nov 6:193:118716. PMID: 41202420
Research Square Preprint

2024 Oct 10.

Solvent & 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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1718 mL

10.8589 mL

21.7179 mL

5 mM

0.4344 mL

2.1718 mL

4.3436 mL

10 mM

0.2172 mL

1.0859 mL

2.1718 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.43 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Cell Assay^[1]

PC-3 (p53^-/-) human androgen-nonresponsive prostate cancer cells are cultured in RPMI 1640 supplemented with 10% fetal bovine serum (FBS) at 37°C in a humidified incubator containing 5% CO₂. The effect of Celecoxib and its derivatives (e.g., OSU-03012) (2.5 μM, 5 μM, 7.5 μM and 10 μM) on PC-3 cell viability is assessed by using the MTT assay in six replicates. Cells are grown in 10% FBS- supplemented RPMI 1640 in 96-well, flat-bottomed plates for 24 h, and are exposed to various concentrations of Celecoxib derivatives (e.g., OSU-03012) dissolved in DMSO (final concentration ≤0.1%) in 1% serum-containing RPMI 1640 for different time intervals. Controls receive DMSO vehicle at a concentration equal to that in drug-treated cells. The medium is removed, replaced by 200 μL of 0.5 mg/mL of MTT in 10% FBS-containing RPMI 1640, and cells are incubated in the CO₂ incubator at 37°C for 2 h. Supernatants are removed from the wells, and the reduced MTT dye is solubilized in 200 μL/well DMSO. Absorbance at 570 nm is determined on a plate reader^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]

Mice^[2]
SCID/Rag2m mice (6-8 weeks old, female) are subcutaneously injected with 1×10⁷ MDA-MB-435/LCC6 cells stably transfected with HER-2/neu. Each mouse is inoculated with the cells on the right and left sides of the lower back. A total of eight mice are injected, each harboring two tumors. After 6 weeks, the mice are randomly assigned into groups (vehicle, 0.5% methyl cellulose/0.1% Tween 80, or OSU-03012 at 200 mg/kg/day). Mice are dosed daily for 3 days with either the vehicle or OSU-03012 by oral gavage. On the fourth day, the study is terminated, mice are sacrificed, and the tumors are collected for chromatin immunoprecipitation (ChIP) and protein isolations.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Zhu J, et al. From the cyclooxygenase-2 inhibitor celecoxib to a novel class of 3-phosphoinositide-dependent protein kinase-1 inhibitors. Cancer Res. 2004 Jun 15;64(12):4309-18. [Content Brief]

[2]. To K, et al. The phosphoinositide-dependent kinase-1 inhibitor 2-amino-N-[4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-acetamide (OSU-03012) prevents Y-box binding protein-1 from inducing epidermal growth factor receptor. Mol Pharmacol. 2007 Sep;72(3):641-52. [Content Brief]

[3]. Tina X Lee, et al.Growth Inhibitory and Anti-Tumour Activities of OSU-03012, a Novel PDK-1 Inhibitor, on Vestibular Schwannoma and Malignant Schwannoma Cells. Eur J Cancer [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1718 mL	10.8589 mL	21.7179 mL	54.2947 mL
	5 mM	0.4344 mL	2.1718 mL	4.3436 mL	10.8589 mL
	10 mM	0.2172 mL	1.0859 mL	2.1718 mL	5.4295 mL
	15 mM	0.1448 mL	0.7239 mL	1.4479 mL	3.6196 mL
	20 mM	0.1086 mL	0.5429 mL	1.0859 mL	2.7147 mL
	25 mM	0.0869 mL	0.4344 mL	0.8687 mL	2.1718 mL
	30 mM	0.0724 mL	0.3620 mL	0.7239 mL	1.8098 mL
	40 mM	0.0543 mL	0.2715 mL	0.5429 mL	1.3574 mL
	50 mM	0.0434 mL	0.2172 mL	0.4344 mL	1.0859 mL
	60 mM	0.0362 mL	0.1810 mL	0.3620 mL	0.9049 mL
	80 mM	0.0271 mL	0.1357 mL	0.2715 mL	0.6787 mL
	100 mM	0.0217 mL	0.1086 mL	0.2172 mL	0.5429 mL

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OSU-03012

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Glucose Metabolism Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Cell Death Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) OSU-03012

Biological Activity

Chemical Information

Publications (8)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

OSU-03012

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Glucose Metabolism Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Cell Death Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) OSU-03012

Biological Activity

Chemical Information

Publications (8)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

OSU-03012 Related Classifications

HY-10547 Related Classifications