Sotrastaurin (Synonyms: AEB071)

Name: Sotrastaurin
Brand: MedChemExpress
SKU: HY-10343
Rating: 5.0 (21 reviews)

Cat. No.: HY-10343 Purity: 99.71%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

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

Sotrastaurin Chemical Structure

CAS No. : 425637-18-9

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10 mM * 1 mL in DMSO ready for reconstitution	USD 145	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 145	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 209	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 704	In-stock	Estimated Time of Arrival: December 31
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Based on 21 publication(s) in Google Scholar

Other Forms of Sotrastaurin:

Sotrastaurin (Standard) Get quote

18 Publications Citing Use of MCE Sotrastaurin

: 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).

: 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.

: 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.

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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)

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]
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]
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]
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

Molecular Weight

438.48

Formula

C₂₅H₂₂N₆O₂

CAS No.

425637-18-9

Appearance

Solid

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

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 (5.70 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 (5.70 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 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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

Please enter your animal formula composition:

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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: 99.71%

Select Batch:

Data Sheet (294 KB) SDS (644 KB)

COA (264 KB) HNMR (159 KB) RP-HPLC (229 KB) LCMS (374 KB)

Handling Instructions (2659 KB)

References

[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]

Kinase Assay ^[1]	Classical and novel PKC isotypes are assayed by scintillation proximity assay technology. In brief, the assay is performed in 20 mM Tris-HCl buffer, pH 7.4, and 0.1% bovine serum albumin by incubating 1.5 μM of the peptide substrate with 10 μM [³³P]ATP, 10 mM Mg (NO₃)₂, 0.2 mM CaCl₂, and PKC at a protein concentration varying from 25 to 400 ng/mL, and lipid vesicles containing 30 mol% phosphatidylserine, 5 mol% diacylglycerol (DAG), and 65 mol% phosphatidylcholine at a final lipid concentration of 0.5 μM. Incubation is performed for 60 min at room temperature. The reaction is stopped by adding 50 μL of a mixture containing 100 mM EDTA, 200 μM ATP, 0.1% Triton X-100, and 0.375 μg/well streptavidin-coated scintillation proximity assay beads in PBS without Ca²⁺ and Mg²⁺. Incorporated radioactivity is measured in a MicroBetaTrilux counter for 1 min. PKCζ is assayed. In situ Thr-219 autophosphorylation status analysis of PKCθ is done by a phospho-site-specific antibody^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[2]	Cells are plated in a 96-well plate and treated with Sotrastaurin, BYL719 or DMSO at indicated concentrations for a period of 5 days. Viability is assessed using Cell Counting Kit. The Combination Index values are calculated using the CompuSyn software. Briefly explained, the plots generated by the CompuSyn software demonstrate the Y-axis combination index values, where CI<1, =1, and >1 indicate synergism, additive effect, and antagonism, respectively. The X-Axis represents the fractional activity, which reflects the fraction of cells inhibited by the treatments relative to vehicle control. For combination index studies, the concentrations tested included Sotrastaurin (0, 125, 250, 500, 1000 nM) and BYL719 (0, 250, 500, 1000, 2000 nM)^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]^[3]	Mice^[2] 6-8 week nu/nu SCID female mice bearing subcutaneously injected 92.1 tumors (7 mice/group) of 100mm³ diameter are treated with vehicle, Sotrastaurin (80mg/kg/d) TID and or BYL719 orally (50mg/kg/d) QD as single agents and in combination, 5 days/week for 2 weeks. After 2 weeks, two animals from each group are sacrificed and tumors are collected to analyze for Western blot. For Omm1 xenogratfs, 6-8 weeks athymic female mice bearing subcutaneously injected Omm1 tumors (7 mice/group) of 100 mm³ diameter are treated with vehicle, Sotrastaurin (80mg/kg/d) TID and or BYL719 orally (50mg/kg/d) QD as single agents and in combination, 5 days/week for 3 weeks. Tumors are homogenized with grinding resins kits. Tumors are collected to analyze for H&E, and terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) staining. Tumors are measured every 2 to 3 days with calipers, and tumor volumes are calculated. Toxicity is monitored by weight loss. Rats^[3] Male Sprague-Dawley (SD) rats (230-250g) are used throughout.Livers from SD rats are stored at 4C in UW solution for 30h, and then transplanted to SD rats with revascularization. Sotrastaurin (30mg/kg b.i.d. via oral gavage) is used in two treatment protocols. In Gr. I (n=10), liver Sotrastaurin is given to liver donors (90min prior to organ harvest) and OLT recipients (90min prior to the transplant, and for three days post-OLT). In Gr. II (n=6), Sotrastaurin is administered to OLT recipients only (according to Gr. I protocol). Gr. III controls are treated with PBS (n=10). OLT survival is assessed at day 14. Separate cohorts in Gr. I (n=3-4/gr) are sacrificed at 6h and 24h; OLT and peripheral blood samples are collected for analyses. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

Complete Stock Solution Preparation Table

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

Sotrastaurin Related Classifications

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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:

Sotrastaurin425637-18-9AEB071AEB 071AEB-071MARCKSPKCMyristoylated alanine-rich C kinase substrateProtein kinase CInhibitorinhibitorinhibit

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Sotrastaurin (Synonyms: AEB071)

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Other Forms of Sotrastaurin:

Sotrastaurin Related Antibodies

18 Publications Citing Use of MCE Sotrastaurin

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Biological Activity

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References

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Sotrastaurin Related Antibodies

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Complete Stock Solution Preparation Table

Sotrastaurin Related Classifications

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