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 NHT2dphHfW6ldHnvckBCe3OjeR?= NXnmbJpXOTByIH7N M1TwOFMhcA>? Mmr3SG1UVw>? MWfpcohq[mm2czDyVm5CKHO7boTo[ZNqew>? NIfYS3kzPTZ7MUG1PC=>
HUVECs  MmDmSpVv[3Srb36gRZN{[Xl? MmL6OVAxdk1? MkPiNUBp NYrEc3FoWmWmdXPld{BFXFhvVILp[4dmemWmIFXu[I91cGWuaXHsJGR6e2[3bnP0bY9v NFS3OlgzPTZ|NEWzPC=>
A549 MlHuSpVv[3Srb36gRZN{[Xl? M3n0U|AvOcLizszN NEDFZm4zPCCq M3fXO4Rm[3KnYYPld{B1cGVicnXsZZRqfmViUFvDMe6yKGyndnXsJI9vKGOnbHygcYVu[nKjbnWgZ491emWjdHXkJGFUNUmY MYSyOVIyQDF4MR?=
A549 NGL1VlBHfW6ldHnvckBCe3OjeR?= MXGwMlHDqM7:TR?= NXvQ[3BMOjRiaB?= NEP6PGJz\WS3Y3XzJJRp\SCneIDy[ZN{cW:wIHzleoVteyCxZjDNUXAuOixiTV3QMVkh[W6mIHnueIVoemmwIN8yNS=> M2XrN|I2OjF6MU[x
A549 MkDWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoO2NE4yyqEQvF2= MnvONlQhcA>? MVvlcohidmOnczDndo94fGhiaX7obYJqfGmxbjDjc5Rz\WG2ZXSge4l1cCCDUz3JWi=> NYDuTGFwOjV{MUixOlE>
Mel202 NH;NNpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;pNE42KM7:TR?= MWizJIg> M1vDe2ROW09? NFradVRmdmijbnPld{BKWi2rbnT1Z4VlKHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gQ>? M2fCdVI1PTl3M{i1
92.1 NGnlbphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLaNE42KM7:TR?= MkLIN{Bp M{jUbmROW09? M2L1NoVvcGGwY3XzJGlTNWmwZIXj[YQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6 MWCyOFU6PTN6NR?=
OCM3 NY\tNHh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV2wMlUh|ryP NH7CO3o{KGh? NIq3SoJFVVOR MnPY[Y5p[W6lZYOgTXIucW6mdXPl[EBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJk> NXuxTpM1OjR3OUWzPFU>
Mel202 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLwNE42KM7:TR?= NIjZXpY{KGh? MVPEUXNQ M3K0eIlv[3KnYYPld{BKWi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1yqB? NEDZd3UzPDV7NUO4OS=>
92.1 NV32ZphIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mle4NE42KM7:TR?= MXKzJIg> MX3EUXNQ M1jxNolv[3KnYYPld{BKWi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1yqB? NVrhb3IxOjR3OUWzPFU>
OCM3 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF[3RWYxNjVizszN MmfQN{Bp NHXwTHJFVVOR NXvXPJpNcW6lcnXhd4V{KEmULXnu[JVk\WRiY3XscEBkgWOuZTDhdpJme3UEoB?= NGe5N|AzPDV7NUO4OS=>
Jeko-1 NGfMTG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PrXVAuPCEQvF2= NX7HWIFCTE2VTx?= NV3k[Yh{cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M2\Ld|I1OzZ{OUO1
Mino NUfH[G5iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHvRXlSOC12IN88US=> MVvEUXNQ NUDybGJtcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NXnpVGlwOjR|NkK5N|U>
Rec-1 NGLXcFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\KNE01KM7:TR?= M4LzN2ROW09? MXLpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NE\BfZczPDN4MkmzOS=>
SP49 NFfacZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWK2N2JuOC12IN88US=> MnnJSG1UVw>? M4OxWYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MYmyOFM3Ojl|NR?=
Jeko-1 M2i0TmZ2dmO2aX;uJGF{e2G7 M17uVFIvPSEQvF5CpC=> MknVNVIhcA>? NGKycmxFVVOR MlPE[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| NVnvSoVCOjR|NkK5N|U>
Mino MWDGeY5kfGmxbjDBd5NigQ>? MoT6Nk42KM7:TdMg NYfLT|dNOTJiaB?= NYfNeIJbTE2VTx?= MmPl[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| MlLjNlQ{PjJ7M{W=
Rec-1 NWDuN3ZJTnWwY4Tpc44hSXO|YYm= MYSyMlUh|ryPwrC= NF:y[IcyOiCq Mln2SG1UVw>? NIfwSXRld3ewcnXneYxifGW|IF7GMe67SiC2YYLn[ZQh\2WwZYO= Ml7BNlQ{PjJ7M{W=
SP49 NFHRemdHfW6ldHnvckBCe3OjeR?= MmPVNk42KM7:TdMg MXKxNkBp MljVSG1UVw>? MnzV[I94dnKnZ4XsZZRmeyCQRj5OvmIhfGG{Z3X0JIdmdmW| MW[yOFM3Ojl|NR?=
CD3+ T  MoDlSpVv[3Srb36gRZN{[Xl? NGPDRYkxNTVyMDDuUS=> MlqxNUBp NVP6OIJlcW6qaXLpeJMhVkZvzsrCJJBpd3OyaH;yfYxifGmxbjDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NUPBfXJIOjN3N{OyPFM>
Mel202 MmmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLrcVQxNTVizszN NI\rOWw4OiCq NYWzfVdyTE2VTx?= NV\5SXl5cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MVOyNlY2Ozl4OB?=
Omm1.3 NIjzclRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTDVZVqOC13IN88US=> NYDE[m5yPzJiaB?= NIjyXZVFVVOR MVPpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NH\JZ5AzOjZ3M{m2PC=>
92.1 NYr5Xo9HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLHW4sxNTVizszN M{W1NlczKGh? MXPEUXNQ NIj3NYVqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NVjRVlFxOjJ4NUO5Olg>
Mel202 M4DtNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3r1ZVUh|ryP MUCyOEBp Mkj2SG1UVw>? M{jQVYlv\HWlZYOgS|Eh[XK{ZYP0xsA> M4\hN|IzPjV|OU[4
Omm1.3 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4D0Z|Uh|ryP NFv3XHkzPCCq MXXEUXNQ NUH2T2ZDcW6mdXPld{BIOSCjcoLld5TDqA>? NULVZ3p3OjJ4NUO5Olg>
92.1 M37IfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWK1JO69VQ>? NVHIcXNjOjRiaB?= M4fU[GROW09? MUXpcoR2[2W|IFexJIFzemW|dNMg NHrqU4YzOjZ3M{m2PC=>
Mel202 Moj1RZBweHSxc3nzJGF{e2G7 NUTu[VNKPSEQvF2= M1TZOlczKGh? MoHkSG1UVw>? M2jLWYlv\HWlZYOgZZBweHSxc3nzJJNtcWeqdHz5 NVPkSndZOjJ4NUO5Olg>
Omm1.3 Mn7ZRZBweHSxc3nzJGF{e2G7 MWS1JO69VQ>? MnXzO|IhcA>? MnW0SG1UVw>? MnHEbY5lfWOnczDhdI9xfG:|aYO= M2fDZ|IzPjV|OU[4
92.1 MmjURZBweHSxc3nzJGF{e2G7 NVnoNpFzPSEQvF2= NGS0e|I4OiCq NH7zb2xFVVOR NGS5TYdqdmS3Y3XzJIFxd3C2b4Ppd{B{cWewaX\jZY51dHl? NUHmZ5Y6OjJ4NUO5Olg>
Mel202 MX;GeY5kfGmxbjDBd5NigQ>? NH\LWFE2KM7:TR?= M1nhflI1KGh? NEHTR5VqdmirYnn0d{BmgHC{ZYPzbY9vKGGwZDDwbI9{eGixconsZZRqd25ib3[gVGtEKGm|b3\vdo1{ NGfTSFkzOjZ3M{m2PC=>
Omm1.3 MWnGeY5kfGmxbjDBd5NigQ>? MmXQOUDPxE1? MVuyOEBp MlvLbY5pcWKrdIOg[ZhxemW|c3nvckBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIGDLR{Bqe2:ob4Ltdy=> M2rzUlIzPjV|OU[4
92.1 NGi1d5lHfW6ldHnvckBCe3OjeR?= NGG2N5g2KM7:TR?= NVrMWoZpOjRiaB?= MlPwbY5pcWKrdIOg[ZhxemW|c3nvckBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIGDLR{Bqe2:ob4Ltdy=> NH2wfJUzOjZ3M{m2PC=>
HBL1 M1GwUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUGwMlE3NTJyIN88US=> NILwe402KGR? M2Hs[GlEPTB;MD61JO69VQ>? Ml;mNlE{OjR7MkC=
TMD8 NGKwPFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVWwMlE3NTJyIN88US=> MWq1JIQ> NWjUWW9nUUN3ME2wMlIh|ryP MoHVNlE{OjR7MkC=
OCI-Ly10 NX\SUWRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUiwMlE3NTJyIN88US=> MYe1JIQ> MUTJR|UxRTFwMzFOwG0> MmX5NlE{OjR7MkC=
U2932 M1;JN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;sOZp4OC5zNj2yNEDPxE1? NF;INIc2KGR? M3i0fGlEPTB;MUCg{txO MUCyNVMzPDl{MB?=
OCI-Ly3 NWe0R|duT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUGwMlE3NTJyIN88US=> M2HwTFUh\A>? NGj4U2xKSzVy78{eNlAh|ryP NGLNWWIzOTN{NEmyNC=>
SuDHL2 NVnibHJkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLzfo4xNjF4LUKwJO69VQ>? MV:1JIQ> NXvyZWNyUUN3MP-8olIxKM7:TR?= MWeyNVMzPDl{MB?=
SuDHL4 NXXCcYtuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nsOlAvOTZvMkCg{txO MnvGOUBl MlPBTWM2OO,:nkKwJO69VQ>? MlfkNlE{OjR7MkC=
DB M{ezTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PzV|AvOTZvMkCg{txO M4jpb|Uh\A>? NIC4W5FKSzVy78{eNlAh|ryP NEHac2ozOTN{NEmyNC=>
Jurkat IL-2 M2rFSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\BTWM2OD14LkexJOKyKDNwN{[g{txO NXTVTodYOTl7NECyOVk>
PBMC IL-2 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXviNnZpUUN3ME20Mlg1KMLzIEGuO|AhKM7:TR?= NXXkb4NtOTl7NECyOVk>

... 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