克唑替尼|T1661

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價(jià)格	詢價(jià)
包裝	1removed

最小起訂量	1removed
發(fā)貨地	上海
更新日期	2026-05-08

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產(chǎn)品詳情

中文名稱:克唑替尼	英文名稱:Crizotinib
CAS:877399-52-5	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
純度規(guī)格: 99.76%	產(chǎn)品類別: 抑制劑
貨號(hào): T001\|T1661

Product Introduction

Bioactivity

名稱	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.
細(xì)胞實(shí)驗(yàn)	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].
激酶實(shí)驗(yàn)	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].
動(dòng)物實(shí)驗(yàn)	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].
體外活性	方法：HMVEC 內(nèi)皮細(xì)胞用 Crizotinib (0.083-1.33 μmol/L) 處理 7 天，使用顯微鏡觀察形態(tài)。結(jié)果：Crizotinib 在纖維蛋白凝膠中抑制血清刺激的 HMVEC 分支小管形成。[1] 方法：9 種肺癌癥細(xì)胞用 Crizotinib 處理 72 h，使用 Cell Titer-Glo Luminescent Cell Viability Assay 檢測(cè)細(xì)胞活力。結(jié)果：具有 MET 擴(kuò)增的兩種細(xì)胞系，EBC-1 和 H1993 均對(duì) Crizotinib 敏感，IC50 值≤10 nM。相反，Crizotinib 沒有顯著抑制具有 MET 突變 (H2122、H1437 和 H596)、具有 EGFR 突變 (PC9 和 HCC827) 或沒有這種基因擴(kuò)增或突變 (A549 和 H1299) 的癌癥細(xì)胞的增殖。[2]
體內(nèi)活性	方法：為檢測(cè)體內(nèi)抗腫瘤活性，將 Crizotinib (3.125-50 mg/kg) 灌胃給藥給攜帶 GTL-16 異種移植物的 nu/nu 小鼠，每天一次，持續(xù)十一天。結(jié)果：在 50 mg/kg/天的劑量水平下，100% 的腫瘤生長(zhǎng)抑制與持續(xù) 24 小時(shí)的 GTL-16 腫瘤中 c-Met 磷酸化的完全抑制相關(guān)。在 >50mg/kg/天的濃度水平下，未觀察到腫瘤生長(zhǎng)抑制的進(jìn)一步改善。[1]
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
溶解度	DMSO : 34.5 mg/mL (76.61 mM), Sonication and heating are recommended. 10% DMSO+90% Saline : 1 mg/mL (2.22 mM), Solution.
關(guān)鍵字	ROSKinase \| ROS1 \| ROS Kinase \| ROS \| PF02341066 \| PF 02341066 \| Inhibitor \| inhibit \| HGFR \| Crizotinib \| c-Met/HGFR \| cMet/HGFR \| c-Met \| cMet \| Cluster of differentiation 246 \| CD246 \| Autophagy \| Anaplastic lymphoma kinase (ALK) \| Anaplastic lymphoma kinase \| ALK tyrosine kinase receptor \| ALK
相關(guān)產(chǎn)品	Allopurinol \| Kaolin \| Guanidine hydrochloride \| Naringin \| Aceglutamide \| Alginic acid \| Hemin \| Hydroxychloroquine \| Stavudine \| Ethoxyquin \| Paeonol \| Ethyl linoleate
相關(guān)庫(kù)	抑制劑庫(kù) \| 抗癌活性化合物庫(kù) \| 抗癌上市藥物庫(kù) \| 臨床失敗化合物庫(kù) \| 激酶抑制劑庫(kù) \| 抗衰老化合物庫(kù) \| FDA 上市藥物庫(kù) \| 免疫/炎癥分子化合物庫(kù) \| 膜蛋白靶向化合物庫(kù) \| 藥物功能重定位化合物庫(kù) \| FDA 上市激酶抑制劑庫(kù) \| 抗癌臨床化合物庫(kù)

關(guān)鍵字：克唑替尼;PF-02341066;TargetMol

公司簡(jiǎn)介

上海陶術(shù)生物科技有限公司為美國(guó)Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國(guó)波士頓、德國(guó)慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實(shí)體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個(gè)性化定制合成；從對(duì)明確靶點(diǎn)的分子篩選到對(duì)明確分子的多靶點(diǎn)篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過在中國(guó)市場(chǎng)五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

成立日期	2013-04-18 （14年）	注冊(cè)資本	566.2651萬(wàn)人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營(yíng)行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營(yíng)模式	貿(mào)易,試劑,定制,服務(wù)

TargetMol中國(guó)（陶術(shù)生物）

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公司成立：14年
注冊(cè)資本：566.2651萬(wàn)人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營(yíng)產(chǎn)品：小分子抑制劑，藥物篩選化合物庫(kù)，天然產(chǎn)物，活性分子化合物等
公司地址：上海市閘北區(qū)江場(chǎng)三路28號(hào)4樓

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