型号:
产品价格:电议      采购度:154      原产地:美洲
发布时间:2023/10/8 9:16:01 所属地区:国外 国外
简要描述:
Akt1/Akt2-IN-1 (Compound 17) 是一种有效的变构抑制剂,抑制 Akt1 (IC50= nM) 和 Akt2 (IC50=42 nM)。
标签:akt2
产品详情
MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务。
CAS No. : 893422-47-4
MCE 站:Akt1/Akt2-IN-1
产品活性:Akt1/Akt2-IN-1 (Compound 17) 是一种有效的变构抑制剂,抑制 Akt1 (IC50=3.5 nM) 和 Akt2 (IC50=42 nM)。
研究领域:PI3K/Akt/mTOR
作用靶点:Akt
In Vitro: Consistent with the allosteric mode of inhibition, Akt1/Akt2-IN-1 (Compound 17) is dependent on the PH-domain for Akt inhibition, is selective for Akt1/2 over Akt3 (IC50=1900 nM), and is highly selective over other members of the AGC family of kinases (>50 μM vs PKA, PKC, SGK). Akt1/Akt2-IN-1 has moderate activity in an hERG binding assay (IC50=5610 nM) and is a substrate for human P-glycoprotein.
In Vivo: Akt1/Akt2-IN-1 (Compound 17) is well tolerated in at exposures that provide high levels of Akt1 and 2 inhibition in vivo. Akt1/Akt2-IN-1 has also been shown to inhibit the growth of A2780 tumors in vivo when used as monotherapy. Akt1/Akt2-IN-1 has potent inhibitory activity against Akt1 and 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. Akt1/Akt2-IN-1 shows good pharmacokinetics in rat with a low clearance of 4.6 mL/min/kg and a half-life of 3.8 h. Due to the improved cell potency, physical properties, and rodent pharmacokinetics of Akt1/Akt2-IN-1, tolerability and Akt inhibition are assessed in mice. Using an acute dosing schedule (IP dosing of 50 mg/kg at times 0, 3, and 8 h), administration of Akt1/Akt2-IN-1 is well tolerated in mice and shows high levels of Akt inhibition in mouse lung.
相关产品:Bioactive Compound Library Plus | Kinase Inhibitor Library | PI3K/Akt/mTOR Compound Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Differentiation Inducing Compound Library | Oxygen Sensing Compound Library | Glycolysis Compound Library | Cytoskeleton Compound Library | Glutamine Metabolism Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Anti-Obesity Compound Library | Angiogenesis-Related Compound Library | Glucose Metabolism Compound Library | Anti-Liver Cancer Compound Library | Anti-Colorectal Cancer Compound Library | Anti-Prostate Cancer Compound Library | Anti-Pulmonary Fibrosis Compound Library | Cancer Stem Cells Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | Serine/Threonine Kinase Inhibitor Library | LM22B-10 | Insulin Detemir | (rac)-AG-205 | Multi-kinase-IN-2 | Akt/SKG Substrate Peptide | AS1949490 | 1,3-Dicaffeoylquinic acid | Threo-Chloramphenicol-d6 | AKT-IN-14 | NSC45586 | APN/AKT-IN-1 | MS5033 | Sophocarpine monohydrate | MS143 | Deferoxamine | Chaetominine | Hu7691 free base | AKT-IN-3 | 8-Aminoadenosine | Nrf2/HO-1 activator 2 | AT13148 | Pachymic acid | Polygalasaponin F | Akt1&PKA-IN-1 | Triciribine | PI3K-IN-29 | Oxaprozin | CCT128930 | YS-49
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides | Antibodies | Click Chemistry
品牌介绍:
• MCE (MedChemExpress) 拥有200 多种全球独家化合物库,我们致力于为全球科研客户提供前沿*全的高品质小分子活性化合物;
• 50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领;
• 产品种类涵盖各种重组蛋白,多肽,常用试剂盒 ,更有 PROTAC、ADC 等特色产品,广泛应用于新药研发、生命科学等科研项目;
• 提供虚拟筛选,离子通道筛选,代谢组学分析检测分析,药物筛选等专业技术服务;
• 设有专业的实验中心和严格的质控、验证体系;
• 提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告,确保产品的高纯度、高品质;
• 产品的生物活性多经各国客户实验验证;
• Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果;
• 专业团队跟踪*新的制药及生命科学研究进展,为您提供全球*新的活性化合物;
• 与世界各大制药公司及知名科研机构建立了长期的合作。
更新时间:2024/1/2 10:31:20
留言咨询
温馨提示
1.遵守中华人民共和国有关法律、法规,尊重网上道德,承担一切因您的行为而直接或间接引起的法律责任。
2.请您真实的反映产品的情况,不要捏造、诬蔑、造谣。如对产品有任何疑问,也可以留言咨询。
3.未经本站同意,任何人不得利用本留言簿发布个人或团体的具有广告性质的信息或类似言论。
相关新闻
相关产品