型号:
产品价格:电议      采购度:1588      原产地:美洲
发布时间:2021/8/2 15:25:52 所属地区:上海 上海市
简要描述:
Nilotinib monohydrochloride monohydrate 是一种二代酪氨酸酶抑制剂,有效抑制 BCR-ABL 及其突变体。
标签:Tasigna
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. : 923288-90-8
MCE 站:Nilotinib monohydrochloride monohydrate
产品活性:Nilotinib monohydrochloride monohydrate 是一种二代酪氨酸酶抑制剂,有效抑制 BCR-ABL 及其突变体。
研究领域:Protein Tyrosine Kinase/RTK | Autophagy
In Vitro: The novel, selective Abl inhibitor, Nilotinib (AMN107), is designed to interact with the ATP-binding site of BCR-ABL with a higher affinity than Imatinib. In addition to being significantly more potent compared with Imatinib (IC50<30 nM), Nilotinib also maintains activity against most of the BCR-ABL point mutants that confer Imatinib resistance. Nilotinib demonstrates significant antitumor efficacy against GIST xenograft lines and Imatinib-resistant GIST cell lines. The parent cell lines GK1C and GK3C show Imatinib sensitivity with IC50 of 4.59±0.97 ?M and 11.15±1.48 ?M, respectively. The Imatinib-resistant cell lines GK1C-IR and GK3C-IR show Imatinib resistance with IC50 values of 11.74±0.17 ?M (P<0.001) and 41.37±1.07 ?M (P<0.001), respectively.
In Vivo: The percentage of tumor growth inhibition (TGI) is 83.8% for Imatinib and 69.6% for Nilotinib in the GK1X xenograft line (n.s.). In the GK2X xenograft line, TGI is 83.0% for Imatinib and 85.3% for Nilotinib (n.s.). Additionally, the GK3X xenograft line TGI is 31.1% for Imatinib and 47.5% for Nilotinib (n.s.). These results suggest that, except for the GK1X xenograft line, Nilotinib shows equivalent or higher antitumor effects than Imatinib. Nilotinib has a significant healing effect on the macroscopic and microscopic pathologic scores and ensures considerable mucosal healing in the indomethacin-induced enterocolitis rat model. While Nilotinib decreased the PDGFR α and β levels and apoptotic scores in the colon, it did not have a significant effect on the weight and TNF-α levels. Further experimental investigations could provide more definitive evidence for humans.
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 | Autophagy Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Cytoskeleton Compound Library | Orally Active Compound Library | FDA Approved & Pharmacopeial Drug Library | Drug-Induced Liver Injury (DILI) Compound Library | Anti-Blood Cancer Compound Library | Nocodazole | Imatinib | Bosutinib | AT9283 | KW-2449 | Bafetinib | DPH | AST 487 | PD173955 | GNF-7 | GNF-5 | GMB-475 | GNF-2 | Lyn-IN-1 | DB07107 | SNIPER(ABL)-020 | CHMFL-ABL/KIT-155 | CT-721 | Imatinib D4 | Imatinib D8 | Multi-kinase inhibitor 1 | ON 146040 | PD180970 | Pivanex | PROTAC BCR-ABL1 ligand 1 | BCR-ABL-IN-1 | SNIPER(ABL)-013 | SNIPER(ABL)-015
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。
更新时间:2024/1/2 10:17:29
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