Art. -Nr.: HY-10343

Sotrastaurin

Name: Sotrastaurin
Brand: MedChemExpress
SKU: HY-10343
Price: 132.00 USD
Availability: InStock
Rating: 5 (24 reviews)

(Synonyms: AEB071)

24 Cited Publications

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Based on 24 publication(s) in Google Scholar

Sotrastaurin (AEB071) is a potent and orally-active pan-PKC inhibitor, with K_is of 0.22 nM, 0.64 nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively.

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Reinheit : 99.79%
CAS. Nr.: 425637-18-9
Formel: C₂₅H₂₂N₆O₂
Molecular Weight:438.48

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Sotrastaurin Chemical Structure

CAS. Nr.: 425637-18-9

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (24)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

PKCθ

0.22 nM (Ki)

PKCβI

0.64 nM (Ki)

PKCα

0.95 nM (Ki)

PKCη

1.8 nM (Ki)

PKCδ

2.1 nM (Ki)

PKCε

3.2 nM (Ki)

Alle PKC Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>3.2 μM Compound: Sotra	Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 33100009]
ASPC1	IC₅₀	>3.2 μM Compound: Sotra	Cytotoxicity in human ASPC1 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Cytotoxicity in human ASPC1 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 33100009]
Bone marrow cell	IC₅₀	3.7 μM Compound: 1	Antiproliferative activity against CBA mouse bone marrow cells assessed as inhibition of [3H]thymidine incorporation after 4 days Antiproliferative activity against CBA mouse bone marrow cells assessed as inhibition of [3H]thymidine incorporation after 4 days	[PMID: 19827831]
BXPC-3	IC₅₀	>3.2 μM Compound: Sotra	Cytotoxicity in human BXPC-3 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Cytotoxicity in human BXPC-3 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 33100009]
Huh-7	CC₅₀	>50 μM Compound: 47	Cytotoxicity against human Huh-7 cells Cytotoxicity against human Huh-7 cells	[PMID: 32283298]
Jurkat	IC₅₀	54 nM Compound: 1	Inhibition of TCR/CD28-mediated human T cell activation in Jurkat cells expressing human IL2 promoter by luciferase reporter gene assay Inhibition of TCR/CD28-mediated human T cell activation in Jurkat cells expressing human IL2 promoter by luciferase reporter gene assay	[PMID: 19827831]
Jurkat	IC₅₀	54 nM Compound: 1, STN, AEB071, sotrastaurin	Inhibition of human Jurkat cell activation assessed as TCR/CD28 stimulated inhibition of IL-2 secretion Inhibition of human Jurkat cell activation assessed as TCR/CD28 stimulated inhibition of IL-2 secretion	[PMID: 21797275]
Lymphocyte	IC₅₀	150 nM Compound: 1, STN, AEB071, sotrastaurin	Immunosuppressive activity in mouse lymphocytes assessed as alloantigen-induced T cell proliferation by mixed lymphocyte reaction assay Immunosuppressive activity in mouse lymphocytes assessed as alloantigen-induced T cell proliferation by mixed lymphocyte reaction assay	[PMID: 21797275]
Lymphocyte	IC₅₀	37 nM Compound: 1, STN, AEB071, sotrastaurin	Immunosuppressive activity in human lymphocytes assessed as alloantigen-induced T cell proliferation by mixed lymphocyte reaction assay Immunosuppressive activity in human lymphocytes assessed as alloantigen-induced T cell proliferation by mixed lymphocyte reaction assay	[PMID: 21797275]
MGC-803	IC₅₀	>3.2 μM Compound: Sotra	Cytotoxicity in human MGC-803 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Cytotoxicity in human MGC-803 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 33100009]
NCI-H1299	IC₅₀	>3.2 μM Compound: Sotra	Cytotoxicity in human NCI-H1299 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Cytotoxicity in human NCI-H1299 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 33100009]
NCI-H1975	IC₅₀	>3.2 μM Compound: Sotra	Cytotoxicity in human NCI-H1975 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Cytotoxicity in human NCI-H1975 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 33100009]
PBMC	IC₅₀	28 nM Compound: Sotrastaurin	Inhibition of human PBMC proliferation assessed as decrease in [3H]-TdR uptake after 6 days by mixed lymphocyte reaction assay Inhibition of human PBMC proliferation assessed as decrease in [3H]-TdR uptake after 6 days by mixed lymphocyte reaction assay	[PMID: 28131714]
PC-9	IC₅₀	>3.2 μM Compound: Sotra	Cytotoxicity in human PC-9 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Cytotoxicity in human PC-9 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 33100009]
RKO	IC₅₀	>3.2 μM Compound: Sotra	Cytotoxicity in human RKO cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Cytotoxicity in human RKO cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 33100009]
SK-MEL-28	IC₅₀	>10 μM Compound: AEB071	Cytotoxicity against human SK-MEL-28 cells expressing B-Raf V600E mutant Cytotoxicity against human SK-MEL-28 cells expressing B-Raf V600E mutant	[PMID: 38198520]
Splenocyte	IC₅₀	128 nM Compound: 1	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay	[PMID: 19827831]
Splenocyte	IC₅₀	34 nM Compound: 1	Immunosuppressive activity in human splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay Immunosuppressive activity in human splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay	[PMID: 19827831]
Vero	CC₅₀	66 μM Compound: 210	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured on day 5 post dose by MTS/PMS based microscopic analysis Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured on day 5 post dose by MTS/PMS based microscopic analysis	[PMID: 28689975]

In Vitro

In cell-free kinase assays Sotrastaurin (AEB071) inhibits PKC, with K_i values in the subnanomolar to low nanomolar range. When Sotrastaurin is tested on a selected panel of kinases, the only enzyme on which Sotrastaurin displays an IC₅₀value below 1 μM is glycogen synthase kinase 3β^[1]. Sotrastaurin (AEB071) inhibits p-MARCKS, a PKC substrate, and pS6 in all the cell lines, independently of the mutational status. There is a slight inhibition of pERK at lower doses also in the GNA11 mutant cells, but not in the WT cells at any concentrations. This is consistent with previous reports indicating that Sotrastaurin inhibits ERK1/2 phosphorylation in GNAQ mutant cell lines^[2].

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

In Vivo

The combination therapy results in a significantly enhanced reduction in tumor volume when compared to either Sotrastaurin (AEB071) or BYL719 alone (p=0.049 vs. BYL719 and p=0.022 vs. Sotrastaurin at day 26). There is even a greater effect when compared to vehicle control (p=0.016)^[2]. Sotrastaurin (STN) treatment of liver donors and orthotopic liver transplantation (OLT) recipients (Gr.I) or of OLT recipients alone (Gr.II) prolongs animal survival, as 9 out of 10 rats in Gr. I, and 6 out of 6 rats in Gr.II survive >14 days. In contrast, only 4 out of 10 control OLT recipients remain alive at day 14 (p<0.01)^[3].

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. Nr. 425637-18-9
Appearance Solid
Molecular Weight 438.48
Formel C₂₅H₂₂N₆O₂
SMILES

O=C(C(C1=C2C=CC=CC2=NC(N3CCN(C)CC3)=N1)=C4C5=CNC6=C5C=CC=C6)NC4=O
Synonyms

AEB071
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (24)

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Journal Impact Factor

Signal Transduct Target Ther

Phosphoglycerate dehydrogenase stabilizes protein kinase C delta type mRNA to promote hepatocellular carcinoma progression. [Abstract]

2025 Jul 18;10(1):236. PMID: 40681503
Cancer Res

The PKC/NF-κB signaling pathway induces APOBEC3B expression in multiple human cancers. [Abstract]

2015 Nov 1;75(21):4538-47. PMID: 26420215

Sotrastaurin purchased from MedChemExpress. Usage Cited in: Cancer Res. 2015 Nov 1;75(21):4538-47. [Abstract]

AEB071 downregulates APOBEC3B in multiple cancer cell lines. The histogram reports APOBEC3B mRNA levels normalized to the vehicle treated control for each line. The dotted line represents a 50% decrease of APOBEC3B expression due to AEB071. The corresponding immunoblots show APOBEC3B and TUBULIN levels. Each line is treated with AEB071 (10 μM) or vehicle control for 48 hours prior to mRNA and protein analysis.
Nat Commun

INSIG1/2 succination mediated by the moonlighting function of ADSL promotes lipogenesis and liver tumorigenesis. [Abstract]

2026 Mar 15;17(1):4002. PMID: 41833955
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
Cell Death Differ

SUMOylation-stabilized G6PD orchestrates metabolic rewiring for oxidative stress survival and chemoresistance in HCC via a PKCδ-phosphorylation trigger. [Abstract]

2026 Jun 26. PMID: 42362742
Mol Ther Oncolytics

APOBEC3 Mediates Resistance to Oncolytic Viral Therapy. [Abstract]

2018 Aug 29:11:1-13. PMID: 30294666

Sotrastaurin purchased from MedChemExpress. Usage Cited in: Mol Ther Oncolytics. 2018 Aug 29:11:1-13. [Abstract]

Levels of murine APOBEC3 are measured by ELISA (left panel) and western blot (right panel) from B16 cells infected with VSV-GFP at an MOI of 0.01 at 0, 48, or 96 hr after treatment with a control IgG, a polyclonal anti-IFN-β antibody, or AEB071 (10 μM).
NPJ Breast Cancer

Clonal heterogeneity in ER+ breast cancer reveals the proteasome and PKC as potential therapeutic targets. [Abstract]

2023 Dec 2;9(1):97. PMID: 38042915
Antioxidants (Basel)

Glucose Activates Lysine-Specific Demethylase 1 through the KEAP1/p62 Pathway. [Abstract]

2021 Nov 26;10(12):1898. PMID: 34942999
Cell Rep

Biased signaling by mutant EGFR underlies dependence on PKCα in lung adenocarcinoma. [Abstract]

2024 Dec 3;43(12):115026. PMID: 39630579
Cell Syst

A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]

2018 Apr 25;6(4):424-443.e7. PMID: 29655704
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
Cancers (Basel)

PKCθ Regulates Pituitary Adenoma Bone Invasion by Activating Osteoclast in NF-κB/IL-1β-Dependent Manner. [Abstract]

2023 Mar 6;15(5):1624. PMID: 36900414
Mol Cell Biochem

Tectoridin inhibits the progression of colon cancer through downregulating PKC/p38 MAPK pathway. [Abstract]

2021 Jul;476(7):2729-2738. PMID: 33683556
Microbiol Spectr

Protein Kinase C Inhibitors Reduce SARS-CoV-2 Replication in Cultured Cells. [Abstract]

2022 Oct 26;10(5):e0105622. PMID: 36000889
bioRxiv

2026 Jul 3.
State University of New York at Stony Brook

2025.
bioRxiv

Nerve Growth Factor Signaling Tunes Axon Maintenance Protein Abundance and Kinetics of Wallerian Degeneration. [Abstract]

2025 Jan 1:2024.12.31.630780. PMID: 39803444
Ruperto Carola University Heidelberg

2023 Jun 1.
bioRxiv

2023 May 28.
Research Square Preprint

2023 May 25.
J Pers Med

GPR30 Activation by 17β-Estradiol Promotes p62 Phosphorylation and Increases Estrogen Receptor α Protein Expression by Inducing Its Release from a Complex Formed with KEAP1. [Abstract]

2021 Sep 11;11(9):906. PMID: 34575683
Patent

20200197325A1
Biomed Pharmacother

Sotrastaurin attenuates the stemness of gastric cancer cells by targeting PKCδ. [Abstract]

2019 Sep:117:109165. PMID: 31261030
Patent

US20180185302A1.

Sotrastaurin purchased from MedChemExpress. Usage Cited in: Patent. US20180185302A1.

Representative PKC inhibitor treated cancer cell line experiment. Each line is treated with AEB071 (10 μM) or vehicle control for 48 hours prior to analysis. The histogram reports APOBEC3B mRNA levels normalized to the vehicle treated control for each line.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 50 mg/mL (114.03 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

2.2806 mL

11.4030 mL

22.8061 mL

5 mM

0.4561 mL

2.2806 mL

4.5612 mL

10 mM

0.2281 mL

1.1403 mL

2.2806 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.70 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.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (294 KB)
SDS (584 KB)
- English - EN (584 KB)
- Français - FR (584 KB)
- Deutsch - DE (584 KB)
- Norwegian - NO (584 KB)
- Español - ES (584 KB)
- Swedish - SV (584 KB)
- Italian - IT (584 KB)
- Korean - KR (584 KB)
- Portuguese - PT (584 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)

Verweise

[1]. Evenou JP, et al. The potent protein kinase C-selective inhibitor AEB071 (sotrastaurin) represents a new class of immunosuppressive agents affecting early T-cell activation. J Pharmacol Exp Ther. 2009 Sep;330(3):792-801. [Content Brief]

[2]. Musi E, et al. The phosphoinositide 3-kinase α selective inhibitor BYL719 enhances the effect of the protein kinase C inhibitor AEB071 in GNAQ/GNA11-mutant uveal melanoma cells. Mol Cancer Ther. 2014 May;13(5):1044-53 [Content Brief]

[3]. Kamo N, et al. Sotrastaurin, a protein kinase C inhibitor, ameliorates ischemia and reperfusion injury in rat orthotopic liver transplantation. Am J Transplant. 2011 Nov;11(11):2499-507. [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2806 mL	11.4030 mL	22.8061 mL	57.0151 mL
	5 mM	0.4561 mL	2.2806 mL	4.5612 mL	11.4030 mL
	10 mM	0.2281 mL	1.1403 mL	2.2806 mL	5.7015 mL
	15 mM	0.1520 mL	0.7602 mL	1.5204 mL	3.8010 mL
	20 mM	0.1140 mL	0.5702 mL	1.1403 mL	2.8508 mL
	25 mM	0.0912 mL	0.4561 mL	0.9122 mL	2.2806 mL
	30 mM	0.0760 mL	0.3801 mL	0.7602 mL	1.9005 mL
	40 mM	0.0570 mL	0.2851 mL	0.5702 mL	1.4254 mL
	50 mM	0.0456 mL	0.2281 mL	0.4561 mL	1.1403 mL
	60 mM	0.0380 mL	0.1901 mL	0.3801 mL	0.9503 mL
	80 mM	0.0285 mL	0.1425 mL	0.2851 mL	0.7127 mL
	100 mM	0.0228 mL	0.1140 mL	0.2281 mL	0.5702 mL

Bioz

Keywords

Sotrastaurin

24 Cited Publications

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Sotrastaurin

Publications Citing Use of MedChemExpress (MCE) Sotrastaurin

Alle PKC Isoform-spezifische Produkte anzeigen