Sotrastaurin

目录号:S2791 别名: AEB071

Sotrastaurin Chemical Structure

Molecular Weight(MW): 438.48

Sotrastaurin是一种有效的,选择性的泛PKC抑制剂,最有效作用于PKCθ,无细胞试验中Ki为0.22 nM;对PKCζ没有活性。Phase 2。

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RMB 5468.97 现货
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客户使用该产品的3个实验数据:

  • 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.

产品安全说明书

PKC抑制剂选择性比较

生物活性

产品描述 Sotrastaurin是一种有效的,选择性的泛PKC抑制剂,最有效作用于PKCθ,无细胞试验中Ki为0.22 nM;对PKCζ没有活性。Phase 2。
特性 同以往的PKC抑制剂不同,AEB071并不会在激活诱导的细胞死亡模型中增强鼠T细胞原幼细胞的凋亡。
靶点
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)
体外研究

在人和鼠的早期T细胞中,毫微摩尔级浓度的AEB071 (< 10μM)则能有效消除早期T细胞激活的信号如白介素-2分泌物和CD25表达。在没发生非特异性抗增殖的效应的细胞中,AEB071 (200 nM)能抑制CD3/CD28抗体和同种抗原诱导的T瞎报增殖反应。AEB071(<3 μM)可以显著抑制淋巴细胞功能相关抗原1介导的T细胞的粘附作用。[1] AEB071(< 20 μM)特异性地降低CD79突变体ABC DLBCL细胞系的增殖,随之能减少NF-κB信号活性。3 μM 浓度的AEB071可诱导CD79突变细胞在G1阻断和/或细胞坏死。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
T cell NWTxWW9rTnWwY4Tpc44hSXO|YYm= NF;DT3UyODBibl2= MWCzJIg> NGrqTIlFVVOR MoK4bY5pcWKrdIOgdnJPSSC|eX70bIV{cXN? NEDSVmczPTZ7MUG1PC=>
HUVECs  NVXYPHVkTnWwY4Tpc44hSXO|YYm= MoTiOVAxdk1? NGL0TZUyKGh? MXHS[YR2[2W|IFTUXE1VemmpZ3Xy[YQhTW6mb4To[Yxq[WxiRInz[pVv[3Srb36= M1u1WVI2PjN2NUO4
A549 MYTGeY5kfGmxbjDBd5NigQ>? Mn\YNE4yyqEQvF2= MWqyOEBp NEfVZ5Zl\WO{ZXHz[ZMhfGinIILlcIF1cX[nIGDLR{3PuSCuZY\lcEBwdiClZXzsJI1mdWK{YX7lJINwfHKnYYTl[EBCWy2LVh?= NVLMUVVJOjV{MUixOlE>
A549 M1zySmZ2dmO2aX;uJGF{e2G7 NEXQ[pcxNjIEoN88US=> NG\mUYozPCCq NYfUXotPemWmdXPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdHNib3[gUW1RNTJuIF3NVE06KGGwZDDpcpRm\3KrbjFOtlE> NYrnO2hkOjV{MUixOlE>
A549 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX6wMlHDqM7:TR?= NH7jPVYzPCCq NU[0dG86\W6qYX7j[ZMh\3Kxd4ToJIlvcGmkaYTpc44h[2:2cnXheIVlKHerdHigRXMuUVZ? MWKyOVIyQDF4MR?=
Mel202 NWK2TGI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vsdFAvPSEQvF2= MlvtN{Bp M4X0XWROW09? Mn;2[Y5p[W6lZYOgTXIucW6mdXPl[EBz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJk> MXGyOFU6PTN6NR?=
92.1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\zNE42KM7:TR?= NFzvXWY{KGh? NXnjOWNPTE2VTx?= M{HZfIVvcGGwY3XzJGlTNWmwZIXj[YQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6 M13DZ|I1PTl3M{i1
OCM3 NEXITopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvhNE42KM7:TR?= MUGzJIg> NH;UfWRFVVOR M3W4e4VvcGGwY3XzJGlTNWmwZIXj[YQhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6 MUeyOFU6PTN6NR?=
Mel202 NIL3Z|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPoPXIxNjVizszN NYXTVppvOyCq M3fBS2ROW09? Mnr2bY5kemWjc3XzJGlTNWmwZIXj[YQh[2WubDDjfYNt\SCjcoLld5TDqA>? M4fQVFI1PTl3M{i1
92.1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XSd|AvPSEQvF2= MlfyN{Bp NHLldIhFVVOR NWTMXHFLcW6lcnXhd4V{KEmULXnu[JVk\WRiY3XscEBkgWOuZTDhdpJme3UEoB?= M1fGdlI1PTl3M{i1
OCM3 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDUeGV5OC53IN88US=> MVGzJIg> MkT0SG1UVw>? M1G3WYlv[3KnYYPld{BKWi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1yqB? MUCyOFU6PTN6NR?=
Jeko-1 M3;kXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTLZlZpOC12IN88US=> M170UWROW09? M1XjeIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> M{mySlI1OzZ{OUO1
Mino NXHiNmNkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XTZVAuPCEQvF2= MUjEUXNQ NFPlenRqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MWSyOFM3Ojl|NR?=
Rec-1 NFPLXoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzibZQxNTRizszN MoPjSG1UVw>? MorHbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MWKyOFM3Ojl|NR?=
SP49 NVrpOHZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnsNE01KM7:TR?= M{LSSWROW09? NGjw[WVqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NG\pUYozPDN4MkmzOS=>
Jeko-1 NHXmSotHfW6ldHnvckBCe3OjeR?= NXTydG9MOi53IN88UeKh NHnEZlMyOiCq NVi2O|hNTE2VTx?= NE\sSlJld3ewcnXneYxifGW|IF7GMe67SiC2YYLn[ZQh\2WwZYO= MVqyOFM3Ojl|NR?=
Mino NXrweY9lTnWwY4Tpc44hSXO|YYm= NFLpR|IzNjVizszNxsA> M1rSZVEzKGh? M{CxVWROW09? M3\LV4Rwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= NITzc2QzPDN4MkmzOS=>
Rec-1 MX3GeY5kfGmxbjDBd5NigQ>? MYSyMlUh|ryPwrC= NYqyZo5uOTJiaB?= MUDEUXNQ M4HMOIRwf26{ZXf1cIF1\XNiTl[t{tpDKHSjcnfleEBo\W6ncx?= M3Pz[FI1OzZ{OUO1
SP49 MVrGeY5kfGmxbjDBd5NigQ>? MoTnNk42KM7:TdMg M2TNPFEzKGh? MWTEUXNQ MXvkc5dvemWpdXzheIV{KE6ILd86RkB1[XKpZYSg[4Vv\XN? NV65VGN[OjR|NkK5N|U>
CD3+ T  NUX5bXN[TnWwY4Tpc44hSXO|YYm= MkjZNE02ODBibl2= NHjLU2YyKGh? MUTpcohq[mm2czDOSk3PwkJicHjvd5Bpd3K7bHH0bY9vKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NWP5e5BSOjN3N{OyPFM>
Mel202 MlK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYK0WGxIOC13IN88US=> NX\sOIp3PzJiaB?= NIG0V4VFVVOR MkG4bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MVKyNlY2Ozl4OB?=
Omm1.3 MnPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV73NIZrOC13IN88US=> M1fzdFczKGh? MoPKSG1UVw>? M4nMeolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> M{fNR|IzPjV|OU[4
92.1 M4DrSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3roSFAuPSEQvF2= MXK3NkBp NG\HUGtFVVOR NWLpVIl6cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MUWyNlY2Ozl4OB?=
Mel202 M{PhdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PRS|Uh|ryP NUHu[IczOjRiaB?= NWLiXXZuTE2VTx?= MojrbY5lfWOnczDHNUBienKnc4VCpC=> NIrFbmEzOjZ3M{m2PC=>
Omm1.3 NVvaW4JtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVO1JO69VQ>? M1fneVI1KGh? Mlm1SG1UVw>? MV7pcoR2[2W|IFexJIFzemW|dNMg NEfsW|EzOjZ3M{m2PC=>
92.1 M{H0NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M36zcFUh|ryP M4HWPVI1KGh? M1Ht[GROW09? M4LUdIlv\HWlZYOgS|Eh[XK{ZYP0xsA> MUmyNlY2Ozl4OB?=
Mel202 MmrIRZBweHSxc3nzJGF{e2G7 NYT5TpBnPSEQvF2= M{\neFczKGh? NWjaW4pETE2VTx?= NXvlXG1zcW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJk> NFvKeHUzOjZ3M{m2PC=>
Omm1.3 M372U2Fxd3C2b4Ppd{BCe3OjeR?= M3f0bVUh|ryP NV;NR3JrPzJiaB?= NFnaVGVFVVOR MVPpcoR2[2W|IHHwc5B1d3Orcx?= MlfaNlI3PTN7Nki=
92.1 MVHBdI9xfG:|aYOgRZN{[Xl? NUDKd5R6PSEQvF2= NUnYbmpJPzJiaB?= MlrDSG1UVw>? MkHZbY5lfWOnczDhdI9xfG:|aYOgd4lodmmoY3HueIx6 NW[zWVVmOjJ4NUO5Olg>
Mel202 NEfUXHNHfW6ldHnvckBCe3OjeR?= MlvkOUDPxE1? MV[yOEBp Mo\lbY5pcWKrdIOg[ZhxemW|c3nvckBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIGDLR{Bqe2:ob4Ltdy=> NWfWcJFIOjJ4NUO5Olg>
Omm1.3 MmTISpVv[3Srb36gRZN{[Xl? MkPiOUDPxE1? MViyOEBp MnrPbY5pcWKrdIOg[ZhxemW|c3nvckBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIGDLR{Bqe2:ob4Ltdy=> NHrTfpMzOjZ3M{m2PC=>
92.1 M3rzOWZ2dmO2aX;uJGF{e2G7 MkD1OUDPxE1? M3ryclI1KGh? MoXpbY5pcWKrdIOg[ZhxemW|c3nvckBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIGDLR{Bqe2:ob4Ltdy=> M1naeVIzPjV|OU[4
HBL1 NFrre21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzyRYJ{OC5zNj2yNEDPxE1? NIDFNIo2KGR? MmnZTWM2OD1yLkWg{txO NYXW[YNzOjF|MkS5NlA>
TMD8 NHLsOmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3WdFAxOC5zNj2yNEDPxE1? M1\HT|Uh\A>? NH7VW|ZKSzVyPUCuNkDPxE1? NHq5cJkzOTN{NEmyNC=>
OCI-Ly10 M2HUR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoH2NE4yPi1{MDFOwG0> NITufZU2KGR? M1fMTWlEPTB;MT6zJO69VQ>? M2jZdFIyOzJ2OUKw
U2932 NUX0fYxbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoGzNE4yPi1{MDFOwG0> M1rWcFUh\A>? MV3JR|UxRTFyIN88US=> NG\TR4wzOTN{NEmyNC=>
OCI-Ly3 M3LZU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTQNE4yPi1{MDFOwG0> NUXVO4xtPSCm M2rsV2lEPTExvK6yNEDPxE1? Mn\ENlE{OjR7MkC=
SuDHL2 NEjKc4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHPVnlMOC5zNj2yNEDPxE1? MVq1JIQ> M1yyNmlEPTExvK6yNEDPxE1? MnnQNlE{OjR7MkC=
SuDHL4 MoXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLJNE4yPi1{MDFOwG0> M2TyVVUh\A>? M4PON2lEPTExvK6yNEDPxE1? NVLqb4xEOjF|MkS5NlA>
DB NF30SJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVuwMlE3NTJyIN88US=> MnrXOUBl MXnJR|Ux97zgMkCg{txO MVyyNVMzPDl{MB?=
Jurkat IL-2 MlTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2j4SmlEPTB;Nj63NUDDuSB|Lke2JO69VQ>? M37zbVE6QTRyMkW5
PBMC IL-2 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLsTWM2OD12Lki0JOKyKDFwN{CgJO69VQ>? MWOxPVk1ODJ3OR?=

... Click to View More Cell Line Experimental Data

体内研究 AEB071(80 mg/kg) 可以在体内显著抑制SCID的皮下TMD8移植模型肿瘤的生长。[2] 每日两次口服10 mg/kg 和30 mg/kg AEB071,能延长心脏移植的大鼠的存活率,这种作用是剂量依赖抑制免疫力的效应。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

动物实验:[3]
+ 展开
  • Animal Models: 雄性 Wistar/F大鼠
  • Formulation: 生理盐水
  • Dosages: 10 mg/kg 和 30 mg/kg
  • Administration: 口服一次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 87 mg/mL (198.41 mM)
Ethanol 2 mg/mL (4.56 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用:
2% DMSO+30% PEG 300+ddH2O
10mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 438.48
化学式

C25H22N6O2

CAS号 425637-18-9
稳定性 powder
别名 AEB071

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

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

技术支持

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

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

  • 回答:

    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.

PKC Signaling Pathway Map

PKC Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID