当前位置: 易推广 > 生物试剂/抗体/细胞 > 生化试剂 > 其他 > MedChemExpress > 产品展示 > MCE信号通路 > PI3K/Akt/mTOR 信号通路 > Omipalisib
Omipalisib
企业档案
会员类型:会员
已获得易推广信誉 等级评定
(0 -40)基础信誉积累,可浏览访问
(41-90)良好信誉积累,可接洽商谈
(91+ )优质信誉积累,可持续信赖
易推广会员:8年
最后认证时间:
注册号: 【已认证】
法人代表: 【已认证】
企业类型:生产商 【已认证】
注册资金:人民币万 【已认证】
产品数:91228
参观次数:11303243
联系我们
MedChemExpress
电话:021-58955995
联系人:客服部 (请说明是在易推广看到的!谢谢)
手机:13611715263
邮编:201203
邮箱:sales@medchemexpress.cn
地址:上海上海
详细内容
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。
Omipalisib
CAS No. : 1086062-66-9
MCE 站:Omipalisib
产品活性:Omipalisib (GSK2126458) 是一种口服有效的,高选择性的 PI3K 抑制剂,抑制 p110α/β/δ/γ,mTORC1/2 的活性,Ki 值分别为 0.019 nM/0.13 nM/0.024 nM/0.06 nM 和 0.18 nM/0.3 nM。Omipalisib 具有抗癌活性。
研究领域:PI3K/Akt/mTOR | Autophagy
In Vitro: Omipalisib (GSK2126458) potently inhibits the activity of common activating mutants of p110α (E542K, E545K, and H1047R) found in human cancer with Ki?of 8 pM, 8 pM and 9 pM, respectively.?Omipalisib causes a significant reduction in the levels of pAkt-S473 with remarkable potency in T47D and BT474 cells with IC50 of 0.41 nM and 0.18 nM, respectively. Furthermore, Omipalisib (GSK2126458) leads to a G1 cell cycle arrest and produces the inhibitory effect on cell proliferation in a large panel of cell lines, including T47D and BT474 breast cancer lines with IC50 of 3 nM and 2.4 nM, respectively. The combination of Omipalisib or GSK1120212 with Omipalisib enhances cell growth inhibition and decreases S6 ribosomal protein phosphorylation in drug-resistant clones from the A375 BRAF(V600E) and the YUSIT1 BRAF(V600K) melanoma cell lines.?Omipalisib (GSK2126458) potentiates the antiproliferative activity of DDR1-IN-1 in colorectal cancer cell lines.
In Vivo: In a BT474 human tumor xenograft model, Omipalisib (GSK2126458) treatment results in a dose-dependent reduction in pAkt-S473 levels, and exhibits dose-dependent tumor growth inhibition at a low dose of 300 μg/kg. Besides, Omipalisib (GSK2126458) shows low blood clearance and good oral bioavailability in four preclinical species (mouse, rat, dog, and monkey).
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Kinase Inhibitor Library | PI3K/Akt/mTOR Compound Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Antioxidants Compound Library | Differentiation Inducing Compound Library | Reprogramming 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 | Rapamycin | 3-Methyladenine | LY294002 | Wortmannin | Everolimus | MHY1485 | Quercetin | 740 Y-P | 3BDO | Temsirolimus | Salidroside | Torkinib | PI-103 | D-α-Hydroxyglutaric acid disodium | Isorhamnetin | L-Leucine | Recilisib | Autophinib | Dihydromyricetin | AZD 6482 | PI3K-IN-1 | TG100-115 | α-Linolenic acid | TGX-221 | 1-Deoxynojirimycin | YS-49 | AS-605240 | PKI-402 | Disitertide | Erucic acid
品牌介绍:
• MCE (MedChemExpress) 拥有数百种全球独家化合物,我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物;
• 10,000 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域;
• 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。
热门标签:GSK2126458