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.

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In DMSO USD 190 In stock
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3 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.

  • Primary mantle cell lymphoma (MCL) cells respond differentially to sotrastaurin and ibrutinib. Primary MCL cells (MCL01-MCL04) were treated with 3 μmol/l sotrastaurin or 400 nmol/l ibrutinib for 2 h (A) or 22 h (B) followed by a stimulation with 3 μg/ml anti-human IgM antibody for 10 min. Subsequently whole cell lysates were analysed by Western blotting. DMSO, dimethyl sulphoxide.

    Br J Haematol, 2016, 173(3):394-403. Sotrastaurin purchased from Selleck.

Purity & Quality Control

Choose Selective PKC Inhibitors

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 MlfqSpVv[3Srb36gRZN{[Xl? MVixNFAhdk1? MYWzJIg> MXjEUXNQ Mme4bY5pcWKrdIOgdnJPSSC|eX70bIV{cXN? NFjJfWczPTZ7MUG1PC=>
HUVECs  MonJSpVv[3Srb36gRZN{[Xl? NHzlfG42ODCwTR?= MnLXNUBp Ml35VoVlfWOnczDEWHguXHKrZ3fldoVlKEWwZH;0bIVtcWGuIFT5d4Z2dmO2aX;u M1nITlI2PjN2NUO4
A549 NX;U[Hd[TnWwY4Tpc44hSXO|YYm= MnjENE4yyqEQvF2= MVSyOEBp NFXYfJBl\WO{ZXHz[ZMhfGinIILlcIF1cX[nIGDLR{3PuSCuZY\lcEBwdiClZXzsJI1mdWK{YX7lJINwfHKnYYTl[EBCWy2LVh?= MV[yOVIyQDF4MR?=
A549 NGjLe4hHfW6ldHnvckBCe3OjeR?= NWrNd45wOC5zwrFOwG0> MXKyOEBp NITwPZJz\WS3Y3XzJJRp\SCneIDy[ZN{cW:wIHzleoVteyCxZjDNUXAuOixiTV3QMVkh[W6mIHnueIVoemmwIN8yNS=> MmHTNlUzOThzNkG=
A549 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3[2PFAvOcLizszN MWmyOEBp M{XrWoVvcGGwY3XzJIdzd3e2aDDpcohq[mm2aX;uJINwfHKnYYTl[EB4cXSqIFHTMWlX MV[yOVIyQDF4MR?=
Mel202 Ml:2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHONE42KM7:TR?= NYDJTIxqOyCq NV\Oc3hCTE2VTx?= NFrRZ3hmdmijbnPld{BKWi2rbnT1Z4VlKHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gQ>? MViyOFU6PTN6NR?=
92.1 NFfNc5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jJU|AvPSEQvF2= MYqzJIg> MUfEUXNQ NGTEd3FmdmijbnPld{BKWi2rbnT1Z4VlKHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gQ>? MnT3NlQ2QTV|OEW=
OCM3 NX\ZdFg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4OxWVAvPSEQvF2= MkTON{Bp MV\EUXNQ NHfMfndmdmijbnPld{BKWi2rbnT1Z4VlKHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gQ>? MUmyOFU6PTN6NR?=
Mel202 NWfnfJlnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEO1fI8xNjVizszN M3jm[VMhcA>? MXPEUXNQ M2K2N4lv[3KnYYPld{BKWi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1yqB? NWDWZXQxOjR3OUWzPFU>
92.1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nROlAvPSEQvF2= NEDoZWM{KGh? M3\jc2ROW09? MkmxbY5kemWjc3XzJGlTNWmwZIXj[YQh[2WubDDjfYNt\SCjcoLld5TDqA>? NVfEeXVMOjR3OUWzPFU>
OCM3 Mo\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfFUopqOC53IN88US=> NXfCcoZEOyCq NWXmNVJ[TE2VTx?= MXHpcoNz\WG|ZYOgTXIucW6mdXPl[EBk\WyuIHP5Z4xmKGG{cnXzeOKh MkPNNlQ2QTV|OEW=
Jeko-1 M2fHZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\1UXB2OC12IN88US=> NUTnZYFZTE2VTx?= MY\pcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M1zqPVI1OzZ{OUO1
Mino Mmf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGL6XIoxNTRizszN MnPnSG1UVw>? NVTETIgycW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NFP0cYkzPDN4MkmzOS=>
Rec-1 NV:z[HB6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrTc5cxNTRizszN MXnEUXNQ NWjHTmx1cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MWiyOFM3Ojl|NR?=
SP49 NIP4T|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW[wMVQh|ryP M1W0emROW09? M1nmb4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MnLpNlQ{PjJ7M{W=
Jeko-1 NV\sZWtSTnWwY4Tpc44hSXO|YYm= NVKzOo83Oi53IN88UeKh NIm2OWQyOiCq M2rkTWROW09? MUjkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? MYqyOFM3Ojl|NR?=
Mino M3K5XGZ2dmO2aX;uJGF{e2G7 NHz1U5gzNjVizszNxsA> M4TUS|EzKGh? NF\rWpVFVVOR M4TkXIRwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= MYKyOFM3Ojl|NR?=
Rec-1 M{TKSGZ2dmO2aX;uJGF{e2G7 M3K4[FIvPSEQvF5CpC=> MYmxNkBp NULRTo5ZTE2VTx?= M1ny[4Rwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= NGLHdnczPDN4MkmzOS=>
SP49 MUXGeY5kfGmxbjDBd5NigQ>? NYTkPGMxOi53IN88UeKh MV:xNkBp NXriWYtFTE2VTx?= NFj6bVJld3ewcnXneYxifGW|IF7GMe67SiC2YYLn[ZQh\2WwZYO= NVq3cnVKOjR|NkK5N|U>
CD3+ T  NFPTZmFHfW6ldHnvckBCe3OjeR?= NYH1NZRtOC13MECgcm0> M1fJeFEhcA>? MWLpcohq[mm2czDOSk3PwkJicHjvd5Bpd3K7bHH0bY9vKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MXGyN|U4OzJ6Mx?=
Mel202 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHudGcxNTVizszN MkXTO|IhcA>? M4L5NGROW09? NXHuN25kcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M4LlU|IzPjV|OU[4
Omm1.3 NYSwUWRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3qVGF5OC13IN88US=> MXm3NkBp MlXHSG1UVw>? M2rxUIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> M1ftO|IzPjV|OU[4
92.1 NYjOcGVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4C2OVAuPSEQvF2= MknuO|IhcA>? M1nEd2ROW09? NVXvZmN7cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NELz[ZozOjZ3M{m2PC=>
Mel202 Mn7jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrEOUDPxE1? NVfF[mJIOjRiaB?= MoXBSG1UVw>? NXHHfYN4cW6mdXPld{BIOSCjcoLld5TDqA>? M2ThT|IzPjV|OU[4
Omm1.3 NULHdm5iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHhOUDPxE1? NEjLOZEzPCCq NF[0Om9FVVOR NETnXIZqdmS3Y3XzJGcyKGG{cnXzeOKh M4K3cVIzPjV|OU[4
92.1 NEfa[FBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4CxSFUh|ryP NEPCWJEzPCCq NXGydFkzTE2VTx?= NFf3SpRqdmS3Y3XzJGcyKGG{cnXzeOKh MV[yNlY2Ozl4OB?=
Mel202 NGXJbVBCeG:ydH;zbZMhSXO|YYm= NVzB[HYyPSEQvF2= NFrZRlE4OiCq MnnpSG1UVw>? M2fSdYlv\HWlZYOgZZBweHSxc3nzJJNtcWeqdHz5 MXOyNlY2Ozl4OB?=
Omm1.3 M3j5eWFxd3C2b4Ppd{BCe3OjeR?= M4TTTFUh|ryP NIHFNGQ4OiCq NITIZo1FVVOR NY\KV3lWcW6mdXPld{BieG:ydH;zbZM> NIHWfHozOjZ3M{m2PC=>
92.1 NEXXemJCeG:ydH;zbZMhSXO|YYm= MonVOUDPxE1? MX23NkBp Mn24SG1UVw>? NWG2XmptcW6mdXPld{BieG:ydH;zbZMhe2mpbnnmZ4FvfGy7 NF\FR28zOjZ3M{m2PC=>
Mel202 M{[0R2Z2dmO2aX;uJGF{e2G7 NGPQbHE2KM7:TR?= NHq3R|czPCCq MmrQbY5pcWKrdIOg[ZhxemW|c3nvckBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIGDLR{Bqe2:ob4Ltdy=> M{\2PVIzPjV|OU[4
Omm1.3 Mo\lSpVv[3Srb36gRZN{[Xl? NEj1S4c2KM7:TR?= MmPhNlQhcA>? MonXbY5pcWKrdIOg[ZhxemW|c3nvckBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIGDLR{Bqe2:ob4Ltdy=> MX2yNlY2Ozl4OB?=
92.1 Mke3SpVv[3Srb36gRZN{[Xl? NGWy[lA2KM7:TR?= MUCyOEBp NYGwVnN[cW6qaXLpeJMh\XiycnXzd4lwdiCjbnSgdIhwe3Cqb4L5cIF1cW:wIH;mJHBMSyCrc3;mc5Juew>? NVPLZZNOOjJ4NUO5Olg>
HBL1 NIP6U5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV[wMlE3NTJyIN88US=> NF3GOJo2KGR? NVfZSnV2UUN3ME2wMlUh|ryP MWOyNVMzPDl{MB?=
TMD8 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1K5O|AvOTZvMkCg{txO MVO1JIQ> MY\JR|UxRTBwMjFOwG0> NU\x[WZ3OjF|MkS5NlA>
OCI-Ly10 NV;le3VUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX[4Z4V3OC5zNj2yNEDPxE1? NUPn[Yx1PSCm M17GVmlEPTB;MT6zJO69VQ>? M{mxVVIyOzJ2OUKw
U2932 M3jDbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;P[oYxNjF4LUKwJO69VQ>? NEHNbZA2KGR? MnvUTWM2OD1zMDFOwG0> NHHBPIszOTN{NEmyNC=>
OCI-Ly3 NWXYTm5CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDBZ4cxNjF4LUKwJO69VQ>? MVu1JIQ> NFOzVIRKSzVy78{eNlAh|ryP NIHRXpAzOTN{NEmyNC=>
SuDHL2 NX2wepN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW[wMlE3NTJyIN88US=> MUS1JIQ> M3;OZ2lEPTExvK6yNEDPxE1? MXGyNVMzPDl{MB?=
SuDHL4 MmX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF6wRmsxNjF4LUKwJO69VQ>? MVi1JIQ> NVTPbYdxUUN3MP-8olIxKM7:TR?= M4\Y[VIyOzJ2OUKw
DB MkHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUmwMlE3NTJyIN88US=> Mo\1OUBl MVXJR|Ux97zgMkCg{txO NWHae4N1OjF|MkS5NlA>
Jurkat IL-2 NULC[oNHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTZwN{GgxtEhOy55NjFOwG0> Ml3PNVk6PDB{NUm=
PBMC IL-2 MkXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPSTWM2OD12Lki0JOKyKDFwN{CgJO69VQ>? MWGxPVk1ODJ3OR?=

... 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 Insoluble
In vivo Add solvents to the product individually and in order:
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
10mg/mL

* 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
Synonyms AEB071

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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

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Frequently Asked Questions

  • Question 1:

    Could you give me the information about how to prepare Sotrastaurin for oral administration in mice?

  • Answer:

    S2791 Sotrastaurin can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 10 mg/ml as a clear solution which can be used for injection, and in 2% DMSO/corn oil at 10 mg/ml as a suspension for oral administration.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID