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. : 1345847-93-9
MCE 国际站:Altiratinib
产品活性:Altiratinib (DCC-2701) 是多靶点激酶抑制剂,抑制 MET,TIE2,VEGFR2,FLT3,Trk1,Trk2 和 Trk3 的 IC50 值分别为2.7,8,9.2,9.3,0.85,4.6,0.83 nM。
研究领域:Protein Tyrosine Kinase/RTK | Neuronal Signaling
作用靶点:VEGFR | c-Met/HGFR | FLT3 | Trk Receptor
In Vitro: Altiratinib also inhibits MET isoforms METD1228H, MET D1228N, METY1230C, METY1230D, METY1230H, METM1250T with IC50s of 3.6, 1.3, 1.2, 0.37, 1.5 and 6 nM, respectively. Altiratinib inhibits MET phosphorylation with IC50 values of 0.85 and 2.2 nM, respectively. In the U-87 glioblastoma cell line, MET and HGF are both expressed. Altiratinib blocks autocrine activation of MET phosphorylation in these cells (IC50=6.2 nM). Altiratinib potently inhibits cellular proliferation in MET-amplified EBC-1 and MKN-45 cells, as well as TPM3-TRKA fusion KM-12 cells. Activation of MET is known to increase the motility and invasiveness of cancer cells: Altiratinib inhibits HGF-induced A549 cell migration, with an IC50 of 13 nM. Altiratinib also inhibits FLT3-ITD mutant MV-4-11 cell proliferation with an IC50 of 12 nM.
In Vivo: A single oral dose of 30 mg/kg Altiratinib leads to >95% inhibition of MET phosphorylation for the entire 24-hour period. A single 10 mg/kg oral dose of Altiratinib exhibits complete inhibition of MET phosphorylation through 12 hours and 73% inhibition at 24 hours postdose. Altiratinib dosed at 10 mg/kg twice a day leads to a significant 90% decrease in BLI signal. Altiratinib exhibits properties amenable to oral administration and exhibits substantial blood–brain barrier penetration, an attribute of significance for eventual treatment of brain cancers and brain metastases.
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Kinase Inhibitor Library | Neuronal Signaling Compound Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Differentiation Inducing Compound Library | Reprogramming Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Angiogenesis-Related Compound Library | Anti-Liver Cancer Compound Library | Rare Diseases Drug Library | Anti-Colorectal Cancer Compound Library | Anti-Pulmonary Fibrosis Compound Library | Cancer Stem Cells Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | 5α-Hydroxycostic acid | GW806742X hydrochloride | JNJ-47117096 hydrochloride | AMG-208 | Sorafenib-d4 | DS-1205b free base | BMS-690514 | AT9283 | LM22B-10 | (E/Z)-Zotiraciclib | AKN-028 acetate | VEGFR-2-IN-6 | TRK-IN-16 | PROTAC VEGFR-2 degrader-1 | c-Met-IN-1 | Glumetinib | Multi-kinase-IN-2 | Savolitinib | ANA-12 | Sorafenib Tosylate | K00546 | c-Met-IN-11 | ABN401 | BPR1K871 | VEGFR-2-IN-29 | Threo-Chloramphenicol-d6 | Foretinib | ZM323881 hydrochloride | ODM-203 | PF-06733804
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
货号: HY-B0791
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最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 等多种顶级期刊及制药专利收录了MCE客户的科研成果;
• 专业团队跟踪最新的制药及生命科学研究进展,为您提供全球最新的活性化合物;
• 与世界各大制药公司及知名科研机构建立了长期的合作。