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。

Crizotinib hydrochloride

CAS No. : 1415560-69-8

MCE 国际站：Crizotinib hydrochloride

产品活性：Crizotinib hydrochloride (PF-02341066 hydrochloride) 是一种口服生物可用的，具有选择性的 ATP 竞争性双 ALK 和 c-Met 抑制剂，IC₅₀ 分别为 20 和 8 nM。在细胞的实验中，Crizotinib hydrochloride (PF-02341066 hydrochloride) 抑制 NPM-ALK 的酪氨酸磷酸化和 c-Met 的酪氨酸磷酸化，IC₅₀ 分别为 24 和 11 nM。它也是 ROS 原癌基因 1 (ROS1) 抑制剂。Crizotinib hydrochloride (PF-02341066 hydrochloride) 具有有效的肿瘤生长抑制作用。

研究领域：Protein Tyrosine Kinase/RTK  |  Autophagy

作用靶点：Anaplastic lymphoma kinase (ALK)  |  c-Met/HGFR  |  ROS Kinase  |  Autophagy

In Vitro: PF-2341066 displays similar potency against c-Met phosphorylation in mIMCD3 mouse or MDCK canine epithelial cells with IC₅₀ of 5 nM and 20 nM, respectivly. PF-2341066 shows improved or similar activity against NIH3T3 cells engineered to express c-Met ATP-binding site mutants V1092I or H1094R or the P-loop mutant M1250T with IC₅₀ of 19 nM, 2 nM and 15 nM, respectively, compared with NIH3T3 cells expressing wild-type receptor with IC₅₀ of 13 nM. In contrast, a marked shift in potency of PF-2341066 is observed against cells engineered to express c-Met activation loop mutants Y1230C and Y1235D with IC₅₀ of 127 nM and 92 nM, respectively, compared with wild-type receptor. PF-2341066 also potently prevents the phosphorylation of c-Met in NCI-H69 and HOP92 cells, with IC₅₀ of 13 nM and 16 nM, respectively, which express the endogenous c-Met variants R988C and T1010I, respectively.
PF-2341066 also potently inhibits NPM-ALK phosphorylation in Karpas299 or SU-DHL-1 ALCL cells with an IC₅₀ of 24 nM. PF-2341066 potently prevents cell proliferation, which is associated with G(1)-S-phase cell cycle arrest and induction of apoptosis in ALK-positive ALCL cells with IC₅₀ of 30 nM, but not ALK-negative lymphoma cells.

In Vivo: PF-2341066 reveals the ability to cause marked regression of large established tumors (> 600 mm³) in both the 50 mg/kg/day and 75 mg/kg/day treatment cohorts, with a 60% decrease in mean tumor volume over the 43-day administration schedule in the GTL-16 model. In an another study, PF-2341066 displays the ability to completely inhibits GTL-16 tumor growth for >3 months, with only 1 of 12 mice exhibiting a significant increase in tumor growth over the 3-month treatment schedule at 50 mg/kg/day. A significant dose-dependent reduction of CD31-positive endothelial cells is observed at 12.5 mg/kg/day, 25 mg/kg/day, and 50 mg/kg/day in GTL-16 tumors, indicating that inhibition of MVD shows a dose-dependent correlation to antitumor efficacy. PF-2341066 displays a significant dose-dependent reduction of human VEGFA and IL-8 plasma levels in both the GTL-16 and U87MG models. Marked inhibition of phosphorylated c-Met, Akt, Erk, PLCλ1, and STAT5 levels is observed in GTL-16 tumors following p.o. administration of PF-2341066.
Treatment of c-MET-amplified GTL-16 xenografts with 50 mg/kg PF-2341066 elicits tumor regression that is associated with a slow reduction in 18F-FDG uptake and decreases expression of the glucose transporter 1, GLUT-1.

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  |  Drug Repurposing Compound Library  |  Orally Active Compound Library  |  Glutamine Metabolism Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Anti-Lung Cancer Compound Library  |  Drug-Induced Liver Injury (DILI) 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   |  EMA-Approved Drug Library  |  FDA-Approved Anticancer Drug Library  |  Anti-Prostate Cancer Compound Library  |  Non-steroidal Anti-Inflammatory Compound Library  |  Cancer Stem Cells Compound Library  |  Mitochondrial Protection Compound Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  Highly Selective Inhibitors Library  |  Highly Selective Activators Library  |  Cytokine Inhibitors Library  |  Cell Death Library  |  Serine/Threonine Kinase Inhibitor Library  |  Anti-Hematopathy Compound Library  |  Anti-Ovarian Cancer Compound Library  |  Multi-Target Compound Library  |  Bioactive Compound Library Max  |  Anti-Gastric Cancer Compound Library  |  Afatinib  |  Crizotinib  |  Cabozantinib  |  Lorlatinib  |  Ceritinib  |  Capmatinib  |  Entrectinib  |  Alectinib  |  Brigatinib  |  MitoPQ  |  Savolitinib  |  Repotrectinib  |  Foretinib  |  Cucurbitacin B  |  L-Cystine  |  NVP-TAE 684  |  Mefloquine hydrochloride  |  Tivantinib  |  PHA-665752  |  Tepotinib  |  BMS 777607  |  Merestinib  |  GSK1838705A  |  Higenamine hydrochloride  |  Lactacystin  |  Telisotuzumab vedotin  |  CEP-37440

热门产品线：重组蛋白  |  药物筛选  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds

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域；
•   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。