OSU-03012 (Synonyms: AR-12; PDK1 inhibitor AR-12)

Name: OSU-03012
Brand: MedChemExpress
SKU: HY-10547
Rating: 5.0 (4 reviews)

Cat. No.: HY-10547 Purity: 98.88%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

OSU-03012 Chemical Structure

CAS No. : 742112-33-0

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 96	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 192	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 348	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 624	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 4 publication(s) in Google Scholar

4 Publications Citing Use of MCE OSU-03012

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Biological Activity
Protocol
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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]
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	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]
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]
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.

Molecular Weight

460.45

Formula

C₂₆H₁₉F₃N₄O

CAS No.

742112-33-0

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

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

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.88%

Select Batch:

Data Sheet (284 KB) SDS (393 KB)

COA (255 KB) LCMS (94 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]

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

Complete Stock Solution Preparation Table

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

OSU-03012 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

OSU-03012742112-33-0AR-12 PDK1 inhibitor AR-12OSU03012OSU 03012AR12AR 12PDK-1Autophagy3-Phosphoinositide-dependent protein kinase 1Inhibitorinhibitorinhibit

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OSU-03012 (Synonyms: AR-12; PDK1 inhibitor AR-12)

Customer Review

OSU-03012 Related Antibodies

4 Publications Citing Use of MCE OSU-03012

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Biological Activity

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Customer Review

OSU-03012 Related Antibodies

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Complete Stock Solution Preparation Table

OSU-03012 Related Classifications

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