Sotrastaurin (Synonyms: AEB071)

目录号: HY-10343 纯度: 99.71%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Sotrastaurin (AEB071) 是一种口服有效的 pan-PKC 抑制剂，作用于 PKCθ，PKCβ，PKCα，PKCη，PKCδ 和 PKCε，K_i 分别为 0.22 nM，0.64 nM，0.95 nM，1.8 nM，2.1 nM 和 3.2 nM。

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Sotrastaurin Chemical Structure

CAS No. : 425637-18-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1377	In-stock
1 mg	￥569	In-stock
5 mg	￥1252	In-stock
10 mg	￥2046	In-stock
50 mg	现货	询价
100 mg		询价
200 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Sotrastaurin:

Sotrastaurin (Standard) 询价

MCE 顾客使用本产品发表的 18 篇科研文献

: 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.

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKCι

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Sotrastaurin (AEB071) is a potent and orally-active pan-PKC inhibitor, with K_is 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)

细胞效力
(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]

体外研究
(In Vitro)

在无细胞激酶测定中，Sotrastaurin (AEB071) 抑制 PKC，K_i 值在亚纳摩尔到低纳摩尔范围内。当在一组选定的激酶上测试 Sotrastaurin 时，Sotrastaurin 显示 IC₅₀ 值低于 1 μM 的唯一酶是糖原合酶激酶 3β^[1]。
Sotrastaurin (AEB071) 抑制所有细胞系中的 p-MARCKS (一种 PKC 底物) 和 pS6，与突变状态无关。在较低剂量下，在 GNA11 突变细胞中也存在对 pERK 的轻微抑制，但在任何浓度的 WT 细胞中都没有。这与之前的报道一致，表明 Sotrastaurin 抑制 GNAQ 突变细胞系中的 ERK1/2 磷酸化^[2]。

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

体内研究
(In Vivo)

与单独的 Sotrastaurin (AEB071) 或 BYL719 相比，联合疗法导致肿瘤体积显著减少 (p=0.049 对比 BYL719，p=0.022 对比 Sotrastaurin，第 26 天)。与对照控制相比，效果甚至更大 (p=0.016)^[2]。
Sotrastaurin (STN) 处理肝脏供体和原位肝移植 (OLT) 接受者 (Gr.I) 或单独接受 OLT 接受者 (Gr.II) 可延长动物存活期，因为 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 名对照 OLT 接受者中只有 4 名在第 14 天还活着 (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 号

425637-18-9

性状

固体

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 50 mg/mL (114.03 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	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
10 mM	0.2281 mL	1.1403 mL	2.2806 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.70 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.70 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.71%

选择批次：

Data Sheet (666 KB) SDS (644 KB)

COA (209 KB) HNMR (159 KB) RP-HPLC (229 KB) LCMS (374 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Evenou JP, et al. The potent protein kinase C-selective inhibitor AEB071 (sotrastaurin) represents a new class of immunosuppressive agents affecting early T-cell activation. J Pharmacol Exp Ther. 2009 Sep;330(3):792-801. [Content Brief]

[2]. Musi E, et al. The phosphoinositide 3-kinase α selective inhibitor BYL719 enhances the effect of the protein kinase C inhibitor AEB071 in GNAQ/GNA11-mutant uveal melanoma cells. Mol Cancer Ther. 2014 May;13(5):1044-53 [Content Brief]

[3]. Kamo N, et al. Sotrastaurin, a protein kinase C inhibitor, ameliorates ischemia and reperfusion injury in rat orthotopic liver transplantation. Am J Transplant. 2011 Nov;11(11):2499-507. [Content Brief]

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.
参考文献	[1]. Evenou JP, et al. The potent protein kinase C-selective inhibitor AEB071 (sotrastaurin) represents a new class of immunosuppressive agents affecting early T-cell activation. J Pharmacol Exp Ther. 2009 Sep;330(3):792-801. [Content Brief] [2]. Musi E, et al. The phosphoinositide 3-kinase α selective inhibitor BYL719 enhances the effect of the protein kinase C inhibitor AEB071 in GNAQ/GNA11-mutant uveal melanoma cells. Mol Cancer Ther. 2014 May;13(5):1044-53 [Content Brief] [3]. Kamo N, et al. Sotrastaurin, a protein kinase C inhibitor, ameliorates ischemia and reperfusion injury in rat orthotopic liver transplantation. Am J Transplant. 2011 Nov;11(11):2499-507. [Content Brief]

Sotrastaurin 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	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.

Keywords:

Sotrastaurin425637-18-9AEB071AEB 071AEB-071MARCKSPKCMyristoylated alanine-rich C kinase substrateProtein kinase CInhibitorinhibitorinhibit

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Sotrastaurin (Synonyms: AEB071)

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Other Forms of Sotrastaurin:

MCE 顾客使用本产品发表的 18 篇科研文献

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•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 PKC 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

Sotrastaurin 相关分类

完整储备液配制表

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Sotrastaurin (Synonyms: AEB071)

Customer Review

Other Forms of Sotrastaurin:

Sotrastaurin 相关抗体

MCE 顾客使用本产品发表的 18 篇科研文献

Sotrastaurin 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 PKC 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

Sotrastaurin 相关抗体:

摩尔计算器

稀释计算器

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