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 > 蛋白酪氨酸激酶 > Ceritinib dihydrochloride
Ceritinib dihydrochloride
价格:¥电议
品牌名称:$brandModel.Title(进口品牌)型号: 原产地:美洲 发布时间:2021/7/24更新时间:2024/1/2
产品完善度: 访问次数:1599
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:91194
参观次数:10506157
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。
Ceritinib dihydrochloride
CAS No. : 1380575-43-8
MCE 站:Ceritinib dihydrochloride
产品活性:Ceritinib dihydrochloride (LDK378 dihydrochloride) 是一种选择性,口服可生物利用且具有 ATP 竞争性的 ALK 酪氨酸激酶抑制剂,IC50 为 200 pM。Ceritinib dihydrochloride (LDK378 dihydrochloride) 还抑制 IGF-1R,InsR 和 STK22D,IC50 值分别为 8、7 和 23 nM。Ceritinib dihydrochloride (LDK378 dihydrochloride) 显示出良好的抗肿瘤效力。
研究领域:Protein Tyrosine Kinase/RTK
作用靶点:ALK | Insulin Receptor | IGF-1R
In Vitro: Ceritinib (LDK378) shows great anti-proliferative activity in Ba/F3-NPM-ALK and Karpas290 cells with IC50 of 26.0 nM and 22.8 nM, compared with IC50 of 319.5 nM and 2477 nM in Ba/F3-Tel-InsR and Ba/F3-WT cells.
In Vivo: Ceritinib (LDK378) is designed to reduce the possibility of forming reactive metabolites and shows undetectable levels of glutathione (GSH) adducts (<1%) in liver microsomes. Ceritinib (LDK378) has relatively good metabolic stability, with moderate CYP3A4 (Midazolam substrate) inhibition and hERG inhibition. Ceritinib (LDK378) exhibits low plasma clearance in animals (mouse, rat, dog and monkey) compared to liver blood flow, with the oral bioavailability of above 55% in mouse, rat, dog and monkey. Ceritinib (LDK378) induces a dose-dependent growth inhibition and tumor regression in the Karpas299 and H2228 rat xenograft models, with no body-weight loss. Ceritinib (LDK378) shows no impact on insulin levels or plasma glucose utilization in the mouse upon chronic dosing up to 100 mg/kg.
相关产品:Drug Repurposing Compound Library Plus | FDA-Approved Drug Library Plus | FDA-Approved Drug Library Mini | Bioactive Compound Library Plus | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | FDA-Approved Drug Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Differentiation Inducing Compound Library | Endocrinology Compound Library | Anti-COVID-19 Compound Library | Orally Active Compound Library | FDA Approved & Pharmacopeial Drug Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Insulin (human) | Insulin(cattle) | A 83-01 | Picropodophyllin | BMS-536924 | GSK1904529A | MSDC 0160 | AZD-3463 | NVP-TAE 226 | AG1024 | AGL-2263 | S961 TFA | Ginsenoside Rg5 | ALK inhibitor 1 | PQ401 | GIP, human | Kaempferitrin | Rhoifolin | X-376 | ALK inhibitor 2 | HG-14-10-04 | 6-Demethoxytangeretin | NBI-31772 hydrate | GIP (1-30) amide, porcine TFA | GIP (1-30) amide,human acetate | JH-VIII-157-02 | MID-1
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:LDK378 dihydrochloride