Sotrastaurin

Catalog No.S2791 Synonyms: AEB071

Sotrastaurin Chemical Structure

Molecular Weight(MW): 438.48

Sotrastaurin is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM in a cell-free assay; inactive to PKCζ. Phase 2.

Size Price Stock Quantity  
In DMSO USD 190 In stock
USD 170 In stock
USD 670 In stock

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

2 Customer Reviews

  • Lysates from H3122 and MGH006 cells treated with 1 µM PMA in the presence or absence of 0.3 µM sotrastaurin (SOT) were fractionated. Immunoblotting was performed with the indicated antibodies.

    Cancer Cell, 2015, 27(3): 397-408 . Sotrastaurin purchased from Selleck.

    J-Lat A2 cells were stimulated by TPA (10 nM) for 24 h in the presence of the indicated concentrations of AUY922 and sotrastaurin, alone or in combination. Samples were analyzed by FACS and data plotted using MacSynergy II software. (A) Representative McSynergy II plot: areas of the graph above zero indicate an additive or synergistic effect. (B) Representative checkerboard grid used to calculate the plot shown in A.

    Proc Natl Acad Sci USA, 2014, 111(15): E1528-37. Sotrastaurin purchased from Selleck.

Purity & Quality Control

Choose Selective PKC Inhibitors

Click to view more

Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Sotrastaurin is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM in a cell-free assay; inactive to PKCζ. Phase 2.
Features Unlike former PKC inhibitors, Sotrastaurin does not enhance apoptosis of murine T-cell blasts in a model of activation-induced cell death.
Targets
PKCθ [1]
(Cell-free assay)
PKCβ1 [1]
(Cell-free assay)
PKCα [1]
(Cell-free assay)
PKCη [1]
(Cell-free assay)
PKCδ [1]
(Cell-free assay)
0.22 nM(Ki) 0.64 nM(Ki) 0.95 nM(Ki) 1.8 nM(Ki) 2.1 nM(Ki)
In vitro

Sotrastaurin (< 10μM) treatment effectively abrogated at low nanomolar concentration markers of early T-cell activation, such as interleukin-2 secretion and CD25 expression, in primary human and mouse T cells. Sotrastaurin (200 nM) inhibits the CD3/CD28 antibody- and alloantigen-induced T-cell proliferation responses in the absence of nonspecific antiproliferative effects. Sotrastaurin (<3 μM) markedly inhibits lymphocyte function-associated antigen-1-mediated T-cell adhesion. [1] Sotrastaurin(< 20 μM) selectively impair the proliferation of CD79 mutant ABC DLBCL cell lines, correlating with decreased NF-κB signaling avctivity. AEB071 at concentration of 5 μM induces G1 arrest and/or cell death in CD79 mutant cells. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
T cell MnvkSpVv[3Srb36gRZN{[Xl? MnPoNVAxKG6P MnnEN{Bp NG[y[phFVVOR M3W4e4lvcGmkaYTzJJJTVkFic4nueIhme2m| MXqyOVY6OTF3OB?=
HUVECs  MUnGeY5kfGmxbjDBd5NigQ>? M3jOcFUxOG6P NYrpZlQ5OSCq M1[yT3Jm\HWlZYOgSHRZNVS{aXfn[ZJm\CCHbnTveIhmdGmjbDDEfZNnfW6ldHnvci=> NEfG[WMzPTZ|NEWzPC=>
A549 NVzJPWc2TnWwY4Tpc44hSXO|YYm= M3nPU|AvOcLizszN M1HUUlI1KGh? NUXOZVNS\GWlcnXhd4V{KHSqZTDy[YxifGm4ZTDQT2Mu|rFibHX2[Ywhd25iY3XscEBu\W2kcnHu[UBkd3S{ZXH0[YQhSVNvSW[= NIOyS2UzPTJzOEG2NS=>
A549 NFzteoZHfW6ldHnvckBCe3OjeR?= NUHUeGZCOC5zwrFOwG0> Ml7ONlQhcA>? NFLERYJz\WS3Y3XzJJRp\SCneIDy[ZN{cW:wIHzleoVteyCxZjDNUXAuOixiTV3QMVkh[W6mIHnueIVoemmwIN8yNS=> NHf4eoczPTJzOEG2NS=>
A549 NHXMXFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfUblcxNjIEoN88US=> M2mzb|I1KGh? M1;QS4VvcGGwY3XzJIdzd3e2aDDpcohq[mm2aX;uJINwfHKnYYTl[EB4cXSqIFHTMWlX Mo\GNlUzOThzNkG=
Mel202 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH2wTHYxNjVizszN MkW2N{Bp NF3Z[4FFVVOR NHqwfWVmdmijbnPld{BKWi2rbnT1Z4VlKHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gQ>? NWHITZBnOjR3OUWzPFU>
92.1 M3HRVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH75cnAxNjVizszN NYj2b2trOyCq NVfRcIRYTE2VTx?= M4LHcYVvcGGwY3XzJGlTNWmwZIXj[YQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6 MmrkNlQ2QTV|OEW=
OCM3 NU\FZ3oyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWiwMlUh|ryP M1jjbFMhcA>? NUPxNnoxTE2VTx?= NHTMeXZmdmijbnPld{BKWi2rbnT1Z4VlKHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gQ>? NY\OclZuOjR3OUWzPFU>
Mel202 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrZcVUxNjVizszN Mn;IN{Bp MluwSG1UVw>? MmOzbY5kemWjc3XzJGlTNWmwZIXj[YQh[2WubDDjfYNt\SCjcoLld5TDqA>? NX;IdmJvOjR3OUWzPFU>
92.1 NXf3eFFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\TXVMxNjVizszN NEKz[FQ{KGh? MkPZSG1UVw>? M4fObYlv[3KnYYPld{BKWi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1yqB? M3;t[FI1PTl3M{i1
OCM3 Mom3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV[wMlUh|ryP MXGzJIg> M3nDXWROW09? M{PGUYlv[3KnYYPld{BKWi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1yqB? NHzmfIEzPDV7NUO4OS=>
Jeko-1 MnzES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDOXFJIOC12IN88US=> MnHSSG1UVw>? MVrpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NWDZbGhMOjR|NkK5N|U>
Mino M4m2N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HzclAuPCEQvF2= MV3EUXNQ NEThdnNqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NV62cVM6OjR|NkK5N|U>
Rec-1 NFnYOGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4i3V|AuPCEQvF2= MmX6SG1UVw>? MXrpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M2\SUVI1OzZ{OUO1
SP49 MlrMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NED4VlAxNTRizszN MWHEUXNQ MXvpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NWOwfWJoOjR|NkK5N|U>
Jeko-1 NILmVnFHfW6ldHnvckBCe3OjeR?= NIXHe48zNjVizszNxsA> MnLMNVIhcA>? Ml7hSG1UVw>? MUTkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? MX:yOFM3Ojl|NR?=
Mino NUjmT|l2TnWwY4Tpc44hSXO|YYm= MonvNk42KM7:TdMg Mk[1NVIhcA>? MmXQSG1UVw>? M4rwPIRwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= NWX4VZJYOjR|NkK5N|U>
Rec-1 MmGxSpVv[3Srb36gRZN{[Xl? MnmyNk42KM7:TdMg NHPsV|IyOiCq MX7EUXNQ MWHkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? MmHBNlQ{PjJ7M{W=
SP49 NHHEVItHfW6ldHnvckBCe3OjeR?= Mm\UNk42KM7:TdMg NEP1SGkyOiCq NUSwOXhyTE2VTx?= NY\2N4lo\G:5boLl[5Vt[XSnczDOSk3PwkJidHHy[4V1KGenbnXz Ml\TNlQ{PjJ7M{W=
CD3+ T  NWHIc4RETnWwY4Tpc44hSXO|YYm= M2rYe|AuPTByIH7N M4CzSVEhcA>? MVXpcohq[mm2czDOSk3PwkJicHjvd5Bpd3K7bHH0bY9vKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MVKyN|U4OzJ6Mx?=
Mel202 NYezO2g4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHnXW0xNTVizszN M3yyTlczKGh? M{S1OmROW09? NInuR3RqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 M1nvNVIzPjV|OU[4
Omm1.3 NXvLVpA5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nOWlAuPSEQvF2= MUe3NkBp MmXkSG1UVw>? MULpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MVGyNlY2Ozl4OB?=
92.1 M{Xw[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M130eFAuPSEQvF2= NYn6XlJpPzJiaB?= NXzzW25rTE2VTx?= MY\pcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M13qTVIzPjV|OU[4
Mel202 NXvpPIRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1ThOlUh|ryP MYeyOEBp Mnr5SG1UVw>? MmPNbY5lfWOnczDHNUBienKnc4VCpC=> NEXmcYszOjZ3M{m2PC=>
Omm1.3 M2\TOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnlTYZNPSEQvF2= MX[yOEBp NIXaXppFVVOR NF\3WGlqdmS3Y3XzJGcyKGG{cnXzeOKh MUWyNlY2Ozl4OB?=
92.1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LJVlUh|ryP NWrVbFlkOjRiaB?= MXnEUXNQ NInDd5NqdmS3Y3XzJGcyKGG{cnXzeOKh M1LzcFIzPjV|OU[4
Mel202 MV;BdI9xfG:|aYOgRZN{[Xl? NGm3VJk2KM7:TR?= NInMWo04OiCq NXTqfHM5TE2VTx?= MUjpcoR2[2W|IHHwc5B1d3OrczDzcIlocHSueR?= NV3zSllUOjJ4NUO5Olg>
Omm1.3 NF7t[5hCeG:ydH;zbZMhSXO|YYm= NGTFN2I2KM7:TR?= NHnIe484OiCq NVj6VFJTTE2VTx?= NHrhfG5qdmS3Y3XzJIFxd3C2b4Ppdy=> MVeyNlY2Ozl4OB?=
92.1 NELXbVRCeG:ydH;zbZMhSXO|YYm= MkXyOUDPxE1? M{f2R|czKGh? MnHQSG1UVw>? M3rjdYlv\HWlZYOgZZBweHSxc3nzJJNq\26rZnPhcpRtgQ>? NUDXUY9COjJ4NUO5Olg>
Mel202 MmHmSpVv[3Srb36gRZN{[Xl? NELZR5k2KM7:TR?= MX6yOEBp M3\JVYlvcGmkaYTzJIV5eHKnc4Ppc44h[W6mIIDoc5NxcG:{eXzheIlwdiCxZjDQT2MhcXOxZn;ycZM> NITEPWgzOjZ3M{m2PC=>
Omm1.3 M1jkRWZ2dmO2aX;uJGF{e2G7 NF;YSpU2KM7:TR?= MXKyOEBp NES1ZZZqdmirYnn0d{BmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gVGtEKGm|b3\vdo1{ MWWyNlY2Ozl4OB?=
92.1 MULGeY5kfGmxbjDBd5NigQ>? NVLQd|k3PSEQvF2= MYWyOEBp NHz5[4xqdmirYnn0d{BmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gVGtEKGm|b3\vdo1{ MWWyNlY2Ozl4OB?=
HBL1 MlzpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DoflAvOTZvMkCg{txO MXS1JIQ> NGPZNmVKSzVyPUCuOUDPxE1? NHzCT40zOTN{NEmyNC=>
TMD8 M4HjR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlGxNE4yPi1{MDFOwG0> NVXaVVYzPSCm NFvLcXVKSzVyPUCuNkDPxE1? MVmyNVMzPDl{MB?=
OCI-Ly10 MkHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TkclAvOTZvMkCg{txO M1jLO|Uh\A>? MVrJR|UxRTFwMzFOwG0> M1HtdFIyOzJ2OUKw
U2932 NXf4[5FVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV[wMlE3NTJyIN88US=> NEfUVnM2KGR? NVj1eJZmUUN3ME2xNEDPxE1? NWrFN5JGOjF|MkS5NlA>
OCI-Ly3 M3mxRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;RdmwxNjF4LUKwJO69VQ>? NGPS[2I2KGR? MULJR|Ux97zgMkCg{txO MXOyNVMzPDl{MB?=
SuDHL2 NYrsVZRTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX32WYtGOC5zNj2yNEDPxE1? MljhOUBl NFP0PHdKSzVy78{eNlAh|ryP M{fjblIyOzJ2OUKw
SuDHL4 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHDW4h1OC5zNj2yNEDPxE1? MX:1JIQ> M2LLZ2lEPTExvK6yNEDPxE1? NXf1XIhUOjF|MkS5NlA>
DB M4Ljc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TIfFAvOTZvMkCg{txO M33lZlUh\A>? NFTwcoJKSzVy78{eNlAh|ryP NHSySmszOTN{NEmyNC=>
Jurkat IL-2 M1jMW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjsVWxxUUN3ME22MlcyKMLzIEOuO|Yh|ryP NFWybZgyQTl2MEK1PS=>
PBMC IL-2 NIOzOlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH30UoNKSzVyPUSuPFQhyrFiMT63NEAh|ryP NYnVdHJSOTl7NECyOVk>

... Click to View More Cell Line Experimental Data

In vivo Sotrastaurin (80 mg/kg) results in significant inhibition of in vivo tumor growth in a subcutaneous TMD8 xenograft model in SCID. [2] Sotrastaurin orally administrated at 10 mg/kg and 30 mg/kg b.i.d. show a dose-dependent immunosuppressive effect leading to pronounced prolongation of heart allograft survival in rats. [3]

Protocol

Animal Research:[3]
+ Expand
  • Animal Models: male Wistar/F rats
  • Formulation: Saline
  • Dosages: 10 mg/kg and 30 mg/kg
  • Administration: Orally administrated
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 87 mg/mL (198.41 mM)
Ethanol 2 mg/mL (4.56 mM)
Water <1 mg/mL
In vivo 2% DMSO+30% PEG 300+ddH2O 10mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 438.48
Formula

C25H22N6O2

CAS No. 425637-18-9
Storage powder
in solvent
Synonyms AEB071

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01854606 Completed CD79 Mutant or ABC-subtype Diffuse Large B-Cell Lymphoma Novartis Pharmaceuticals|Novartis December 5, 2013 Phase 1|Phase 2
NCT02273219 Recruiting Uveal Melanoma Richard D. Carvajal|Columbia University November 2014 Phase 1
NCT01801358 Terminated Uveal Melanoma Array BioPharma August 2013 Phase 1|Phase 2
NCT01402440 Terminated Diffuse Large B-Cell Lymphoma Novartis Pharmaceuticals|Novartis November 2011 Phase 1
NCT00572585 Completed Ulcerative Colitis Novartis Pharmaceuticals|Novartis April 2010 Phase 2
NCT01128335 Completed Liver Transplantation Novartis Pharmaceuticals|Novartis April 2010 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

PKC Signaling Pathway Map

PKC Inhibitors with Unique Features

Related PKC Products

Tags: buy Sotrastaurin | Sotrastaurin supplier | purchase Sotrastaurin | Sotrastaurin cost | Sotrastaurin manufacturer | order Sotrastaurin | Sotrastaurin distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID