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Sotrastaurin (AEB071)
Sotrastaurin (AEB071) 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。
Sotrastaurin (AEB071) Chemical Structure
CAS: 425637-18-9
产品质控
批次：
纯度：
99.97%
99.97
Sotrastaurin (AEB071)相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息(PMID) |
|---|---|---|---|---|---|
| 92.1 | Growth Inhibition Assay | 0-5 μM | 72 h | inhibits cell growth dose dependently | 22653968 |
| Omm1.3 | Growth Inhibition Assay | 0-5 μM | 72 h | inhibits cell growth dose dependently | 22653968 |
| Mel202 | Growth Inhibition Assay | 0-5 μM | 72 h | inhibits cell growth dose dependently | 22653968 |
| CD3+ T | Function Assay | 0-500 nM | 1 h | inhibits NF-κB phosphorylation in a dose dependent manner | 23573283 |
| SP49 | Function Assay | 2.5 μM | 12 h | downregulates NF-κB target genes | 24362935 |
| Rec-1 | Function Assay | 2.5 μM | 12 h | downregulates NF-κB target genes | 24362935 |
| Mino | Function Assay | 2.5 μM | 12 h | downregulates NF-κB target genes | 24362935 |
| Jeko-1 | Function Assay | 2.5 μM | 12 h | downregulates NF-κB target genes | 24362935 |
| OCM3 | Growth Inhibition Assay | 0.5 μM | 3 h | increases IR-induced cell cycle arrest | 24595385 |
| 92.1 | Growth Inhibition Assay | 0.5 μM | 3 h | increases IR-induced cell cycle arrest | 24595385 |
| Mel202 | Growth Inhibition Assay | 0.5 μM | 3 h | increases IR-induced cell cycle arrest | 24595385 |
| OCM3 | Growth Inhibition Assay | 0.5 μM | 3 h | enhances IR-induced reduction in cell viability | 24595385 |
| 92.1 | Growth Inhibition Assay | 0.5 μM | 3 h | enhances IR-induced reduction in cell viability | 24595385 |
| Mel202 | Growth Inhibition Assay | 0.5 μM | 3 h | enhances IR-induced reduction in cell viability | 24595385 |
| A549 | Growth Inhibition Assay | 0.1 μM | 24 h | enhances growth inhibition cotreated with AS-IV | 25218161 |
| A549 | Function Assay | 0.1 μM | 24 h | reduces the expression levels of MMP-2, MMP-9 and integrin β1 | 25218161 |
| A549 | Function Assay | 0.1 μM | 24 h | decreases the relative PKC-α level on cell membrane cotreated AS-IV | 25218161 |
| HUVECs | Function Assay | 500nM | 1 h | Reduces DTX-Triggered Endothelial Dysfunction | 25634538 |
| T cell | Function Assay | 100 nM | 3 h | inhibits rRNA synthesis | 25691158 |
| Mel202 | Growth Inhibition Assay | 5 μM | 24 h | induces G1 arrest | 22653968 |
| Omm1.3 | Growth Inhibition Assay | 5 μM | 24 h | induces G1 arrest | 22653968 |
| 92.1 | Growth Inhibition Assay | 5 μM | 24 h | induces G1 arrest | 22653968 |
| Mel202 | Apoptosis Assay | 5 μM | 72 h | induces apoptosis slightly | 22653968 |
| Omm1.3 | Apoptosis Assay | 5 μM | 72 h | induces apoptosis | 22653968 |
| 92.1 | Apoptosis Assay | 5 μM | 72 h | induces apoptosis signifcantly | 22653968 |
| Mel202 | Function Assay | 5 μM | 24 h | inhibits expression and phosphorylation of PKC isoforms | 22653968 |
| Omm1.3 | Function Assay | 5 μM | 24 h | inhibits expression and phosphorylation of PKC isoforms | 22653968 |
| 92.1 | Function Assay | 5 μM | 24 h | inhibits expression and phosphorylation of PKC isoforms | 22653968 |
| HBL1 | Growth Inhibition Assay | 0.16-20 μM | 5 d | IC50=0.5 μM | 21324920 |
| TMD8 | Growth Inhibition Assay | 0.16-20 μM | 5 d | IC50=0.2 μM | 21324920 |
| OCI-Ly10 | Growth Inhibition Assay | 0.16-20 μM | 5 d | IC50=1.3 μM | 21324920 |
| U2932 | Growth Inhibition Assay | 0.16-20 μM | 5 d | IC50=10 μM | 21324920 |
| OCI-Ly3 | Growth Inhibition Assay | 0.16-20 μM | 5 d | IC50＞20 μM | 21324920 |
| SuDHL2 | Growth Inhibition Assay | 0.16-20 μM | 5 d | IC50＞20 μM | 21324920 |
| SuDHL4 | Growth Inhibition Assay | 0.16-20 μM | 5 d | IC50＞20 μM | 21324920 |
| DB | Growth Inhibition Assay | 0.16-20 μM | 5 d | IC50＞20 μM | 21324920 |
| SP49 | Growth Inhibition Assay | 0-4 μM | inhibits cell growth dose dependently | 24362935 | |
| Rec-1 | Growth Inhibition Assay | 0-4 μM | inhibits cell growth dose dependently | 24362935 | |
| Mino | Growth Inhibition Assay | 0-4 μM | inhibits cell growth dose dependently | 24362935 | |
| Jeko-1 | Growth Inhibition Assay | 0-4 μM | inhibits cell growth dose dependently | 24362935 | |
| Jurkat T | Function assay | 5 hrs | Inhibition of PKCtheta in human Jurkat T cells assessed as reduction in anti-CD3/CD28 antibody-induced T-cell activation by measuring decrease in IL-2 secretion after 5 hrs by luciferase reporter gene assay, IC50 = 0.081 μM. | 28131714 | |
| bone marrow cells | Antiproliferative assay | 4 days | Antiproliferative activity against CBA mouse bone marrow cells assessed as inhibition of [3H]thymidine incorporation after 4 days, IC50 = 3.7 μM. | 19827831 | |
| Jurkat IL-2 | Growth Inhibition Assay | IC50=6.71 ± 3.76 μM | 19940259 | ||
| PBMC IL-2 | Growth Inhibition Assay | IC50=4.84 ± 1.70 μM | 19940259 | ||
| Jurkat | Function assay | Inhibition of TCR/CD28-mediated human T cell activation in Jurkat cells expressing human IL2 promoter by luciferase reporter gene assay, IC50 = 0.054 μM. | 19827831 | ||
| B-cells | Function assay | Inhibition of PKCbeta in mouse B cells assessed as reduction in IgM-stimulated cell proliferation, IC50 = 0.234 μM. | 28131714 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Sotrastaurin (AEB071) 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 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | 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] |
|||
|---|---|---|---|---|
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | pPKCδ/θ / phosphorylated MARCKS / p53 / MDM2 / PUMA / p21 Cyclin D1 / p27(Kip1) Bcl-xl / XIAP / Survivin PKCα / PKCδ / PKCβ / PKCε / PKCθ p-Marcks / p-ERK / p-AKT / p-S6 / Marcks / ERK / AKT / S6 |
|
29593251 | |
| Growth inhibition assay | Cell viability |
|
22653968 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 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] |
|
|---|---|---|
| 动物实验 | Animal Models | 雄性 Wistar/F大鼠 |
| Dosages | 10 mg/kg 和 30 mg/kg | |
| Administration | 口服一次 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02273219 | Completed | Uveal Melanoma |
Columbia University |
November 19 2014 | Phase 1 |
| NCT01801358 | Terminated | Uveal Melanoma |
Array Biopharma now a wholly owned subsidiary of Pfizer|Array BioPharma |
August 2013 | Phase 1|Phase 2 |
| NCT01430416 | Completed | Uveal Melanoma |
Novartis Pharmaceuticals|Novartis |
December 20 2011 | Phase 1 |
| NCT01402440 | Terminated | Diffuse Large B-Cell Lymphoma |
Novartis Pharmaceuticals|Novartis |
November 2011 | Phase 1 |
|
化学信息&溶解度
| 分子量 | 438.48 | 分子式 | C25H22N6O2 |
| CAS号 | 425637-18-9 | SDF | Download Sotrastaurin (AEB071) SDF |
| Smiles | CN1CCN(CC1)C2=NC3=CC=CC=C3C(=N2)C4=C(C(=O)NC4=O)C5=CNC6=CC=CC=C65 | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 87 mg/mL ( (198.41 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 40 mg/mL (91.22 mM) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解配方 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | |||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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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.
