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  2. Cytoskeleton Epigenetics TGF-beta/Smad
  3. MARCKS PKC
  4. Sotrastaurin

Sotrastaurin (AEB071) 是一種口服有效的 pan-PKC 抑制劑，作用于 PKCθ，PKCβ，PKCα，PKCη，PKCδ 和 PKCε，Ki 分別為 0.22 nM，0.64 nM，0.95 nM，1.8 nM，2.1 nM 和 3.2 nM。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報，我們不為任何個人用途提供產(chǎn)品和服務(wù)

Sotrastaurin Chemical Structure

Sotrastaurin Chemical Structure

CAS No. : 425637-18-9

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2.  同一機(jī)構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機(jī)構(gòu)（單位）一年內(nèi)

     可免費申領(lǐng)三個不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1208
In-stock
1 mg ￥569
In-stock
5 mg ￥1252
In-stock
10 mg ￥2046
In-stock
25 mg ￥4188
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100 mg 現(xiàn)貨 詢價
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Customer Review

Other Forms of Sotrastaurin:

    Sotrastaurin purchased from MCE. 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 MCE. 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 MCE. 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.

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Sotrastaurin (AEB071) is a potent and orally-active pan-PKC inhibitor, with Kis 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[1].

    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)

    細(xì)胞效力
    (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]
    體外研究
    (In Vitro)

    在無細(xì)胞激酶測定中，Sotrastaurin (AEB071) 抑制 PKC，Ki 值在亞納摩爾到低納摩爾范圍內(nèi)。當(dāng)在一組選定的激酶上測試 Sotrastaurin 時，Sotrastaurin 顯示 IC50 值低于 1 μM 的唯一酶是糖原合酶激酶 3β[1]。
    Sotrastaurin (AEB071) 抑制所有細(xì)胞系中的 p-MARCKS (一種 PKC 底物) 和 pS6，與突變狀態(tài)無關(guān)。在較低劑量下，在 GNA11 突變細(xì)胞中也存在對 pERK 的輕微抑制，但在任何濃度的 WT 細(xì)胞中都沒有。這與之前的報道一致，表明 Sotrastaurin 抑制 GNAQ 突變細(xì)胞系中的 ERK1/2 磷酸化[2]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    與單獨的 Sotrastaurin (AEB071) 或 BYL719 相比，聯(lián)合療法導(dǎo)致腫瘤體積顯著減少 (p=0.049 對比 BYL719，p=0.022 對比 Sotrastaurin，第 26 天)。與對照控制相比，效果甚至更大 (p=0.016)[2]。
    Sotrastaurin (STN) 處理肝臟供體和原位肝移植 (OLT) 接受者 (Gr.I) 或單獨接受 OLT 接受者 (Gr.II) 可延長動物存活期，因為 Gr. 10 只大鼠中有 9 只。I 和 Gr.II 中 6 只大鼠中的 6 只存活 > 14 天。相比之下，10 名對照 OLT 接受者中只有 4 名在第 14 天還活著 (p<0.01)[3]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    分子量

    438.48

    Formula

    C25H22N6O2
    CAS 號
    性狀

    固體

    顏色

    Orange to red

    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性數(shù)據(jù)
    細(xì)胞實驗： 

    DMSO 中的溶解度 : ≥ 50 mg/mL (114.03 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制儲備液
    濃度 溶劑體積 質(zhì)量 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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6個月內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗：

    請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.70 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.70 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.79%

    參考文獻(xiàn)
    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.
    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6個月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 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
    Help & FAQs
    • 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.

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    Inquiry Information

    產(chǎn)品名稱：
    Sotrastaurin
    目錄號：
    HY-10343
    需求量：