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  • 克唑替尼|T1661

克唑替尼|T1661

Crizotinib
877399-52-5
￥255 5mg 起订
￥387 10mg 起订
￥555 50mg 起订
上海 更新日期：2024-12-02

TargetMol中国（陶术生物）

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产品详情:

中文名称：
克唑替尼
英文名称：
Crizotinib
CAS号：
877399-52-5
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
99.87%
产品类别：
抑制剂
货号：
T1661

Product Introduction

Bioactivity

名称Crizotinib
描述Crizotinib (PF-02341066) is a small molecule tyrosine kinase inhibitor that inhibits c-MET and ALK receptors (IC50=8/20 nM), is ATP-competitive, and also inhibits ROS1. Crizotinib exhibits antitumor activity and inhibits tumor growth.
细胞实验Cells were seeded in 96-well plates in media supplemented with 10% fetal bovine serum (FBS) and transferred to serum-free media (with 0.04% BSA) after 24 h. In experiments investigating ligand-dependent RTK phosphorylation, corresponding growth factors were added for up to 20 min. After incubation of cells with PF-2341066 for 1 h and/or appropriate ligands for the designated times, cells were washed once with HBSS supplemented with 1 mmol/L Na3VO4, and protein lysates were generated from cells. Subsequently, phosphorylation of selected protein kinases was assessed by a sandwich ELISA method using specific capture antibodies used to coat 96-well plates and a detection antibody specific for phosphorylated tyrosine residues. Antibody-coated plates were (a) incubated in the presence of protein lysates at 4°C overnight; (b) washed seven times in 1% Tween 20 in PBS; (c) incubated in a horseradish peroxidase-conjugated anti–total-phosphotyrosine (PY-20) antibody (1:500) for 30 min; (d) washed seven times again; (e) incubated in 3,3′,5,5′-tetramethylbenzidine peroxidase substrate to initiate a colorimetric reaction that was stopped by adding 0.09 N H2SO4; and (f) measured for absorbance in 450 nm using a spectrophotometer [1].
激酶实验c-Met catalytic activity was quantitated using a continuous-coupled spectrophotometric assay in which the time-dependent production of ADP by c-Met was determined by analysis of the rate of consumption of NADH. NADH consumption was measured by a decrease in absorbance at 340 nm by spectrophotometry at designated time points. To determine Ki values, PF-2341066 was introduced into test wells at various concentrations in the presence of assay reagents and incubated for 10 min at 37°C. The assay was initiated by the addition of the c-Met enzyme [1].
动物实验Daily treatment with PF-2341066 given in water by oral gavage was initiated when tumors were 100 to 600 mm^3 in volume. Tumor volume was determined by measurement with electronic Vernier calipers, and tumor volume was calculated as the product of its length × width2 × 0.4. Tumor volume was expressed on indicated days as the median tumor volume ± SE indicated for groups of mice. Percent (%) inhibition values were measured on the final day of study for drug-treated compared with vehicle-treated mice and are calculated as 100 × {1?[(TreatedFinal day ? TreatedDay 1)/(ControlFinal day ? ControlDay 1)]}. Tumor regression values were determined by calculating the ratio of median tumor volumes at the time when treatment was initiated to the median tumor volume on the final day of study for a given treatment group. Significant differences between the treated versus the control groups (P ≤ 0.001) were determined using one-way ANOVA [1].
体外活性方法：HMVEC 内皮细胞用 Crizotinib (0.083-1.33 µmol/L) 处理 7 天，使用显微镜观察形态。 结果：Crizotinib 在纤维蛋白凝胶中抑制血清刺激的 HMVEC 分支小管形成。[1] 方法：9 种肺癌症细胞用 Crizotinib 处理 72 h，使用 Cell Titer-Glo Luminescent Cell Viability Assay 检测细胞活力。 结果：具有 MET 扩增的两种细胞系，EBC-1 和 H1993 均对 Crizotinib 敏感，IC50 值≤10 nM。相反，Crizotinib 没有显著抑制具有 MET 突变 (H2122、H1437 和 H596)、具有 EGFR 突变 (PC9 和 HCC827) 或没有这种基因扩增或突变 (A549 和 H1299) 的癌症细胞的增殖。[2]
体内活性方法：为检测体内抗肿瘤活性，将 Crizotinib (3.125-50 mg/kg) 灌胃给药给携带 GTL-16 异种移植物的 nu/nu 小鼠，每天一次，持续十一天。 结果：在 50 mg/kg/天的剂量水平下，100% 的肿瘤生长抑制与持续 24 小时的 GTL-16 肿瘤中 c-Met 磷酸化的完全抑制相关。在 >50mg/kg/天的浓度水平下，未观察到肿瘤生长抑制的进一步改善。[1]
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 10 mg/mL (22.21 mM)
10% DMSO+90% Saline : 1 mg/mL (2.22 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
2eq.HCl : 45 mg/mL (100 mM)
关键字Cluster of differentiation 246 | c-Met/HGFR | PF02341066 | Inhibitor | ROS Kinase | Anaplastic lymphoma kinase | inhibit | CD246 | Autophagy | PF 02341066 | ALK tyrosine kinase receptor | Crizotinib | Anaplastic lymphoma kinase (ALK)
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相关库经典已知活性库 | 抗癌活性化合物库 | 已知活性化合物库 | EMA 上市药物库 | 激酶抑制剂库 | FDA 上市药物库 | 酪氨酸激酶分子库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库
克唑替尼|||PF-02341066|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (12年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

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