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Lapatinib (GW-572016) Ditosylate | 购买HER2 抑制剂 - Selleck188bio精品生物—专注于实验室精品爆款的电商平台 - 蚂蚁淘旗下精选188款生物医学科研用品
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Lapatinib (GW-572016) Ditosylate | 购买HER2 抑制剂 - Selleck

定制您的化合物库 通过在我们的库存中挑选化合物来建立合适的化合物库,用于您的研究工作。 您可以选择: 特定化合物 96/384孔板位图 可选择\"干/固体”或\"DMSO溶液” 请通过info@selleck.cn与我们联系,定制你所需要的化合物库。 Lapatinib (GW-572016) Ditosylate是一种有效的EGFR 和 ErbB2抑制剂,在无细胞试验中IC50分别为10.8和9.2 nM。 大剂量询单有大折扣! 今日订购,明日送达,全国免运费!全国免费电话:400-668-6834|Email:info@selleck.cn 产品描述 Lapatinib (GW-572016) Ditosylate是一种有效的EGFR 和 ErbB2抑制剂,在无细胞试验中IC50分别为10.8和9.2 nM。 Lapatinib 微弱抑制ErbB4活性,IC50为367 nM, 作用于EGFR和 ErbB2 比作用于其他激酶,如c-Src, c-Raf, MEK, ERK, c-Fms, CDK1, CDK2, p38, Tie-2,和 VEGFR-2选择性高300多倍。Lapatinib作用于HN5细胞时,显著抑制受体EGFR 和 ErbB2自磷酸化,这种作用存在剂量依赖性,IC50分别为170 nM和80 nM,而作用于BT474细胞时,IC50分别为210 nM 和 60 nM。与OSI-774和Iressa(ZD1839)优先抑制过量表达EGFR细胞生长不同, Lapatinib 抑制过量表达EGFR和ErbB2细胞生长。 作用于过量表达EGFR或 ErbB2的细胞具有高抑制活性,IC50为0.09-0.21 μM,而作用于表达低水平EGFR或ErbB2的细胞,IC50为3-12 μM,比作用于正常纤维细胞选择性高100倍。Lapatinib有效抑制过量表达EGFR的HN5和A-431细胞生长,也抑制过量表达ErbB2的BT474和N87细胞生长,且显著诱导HN5细胞周期停在G1期,也诱导 BT474 细胞凋亡,与抑制AKT磷酸化相关。[1] Lapatinib 作用于含EGFR的L858R和T790M突变的抗Gefitinib的H1975细胞显著抑制Stat3磷酸化,导致细胞生长受抑制,IC50为1-2 μM。[3] NUTIVZpJSW62aYDyc4xqmW{YYTpeoUh[WO2aYpeJkh[WejaX7zeEBpfW2jbjDIUlUh[2WubDDsbY5mNCCLQ{WwQVAvODJ3IN88US= M4jtV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1mC6wY3LpMo5tdS6waXiu[493NzF4NEizO|czLz5zNkS4N|c4OjxxYU6= NIHIc4ZCdnSrcILvcIlnXKjdHn2[UBi[3Srdnn0fUBi2GrboP0JIh2dWGwIFLUOFc1KGOnbHygcIlvSxiSVO1NF0xNjB{NTFOwG0 NHD[Ww9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJuWRwbnPibU5vdG1wbnnoModwfi9zNkS4N|c4Oid-MU[0PFM4PzJ:L3G+ M2LWNWlvcGmkaYTpc44hd2ZiSF61JINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czygTWM2OD1yLkGyJO69VQ ? 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All values are presented as the mean standard error (S.E.) (**p 0.01). Cell viability ; PubMed: 24947784 Oncotarget Huh7 (A), HepG2 (B), or HA22T (C) HCC cells were left untreated or treated with 0.1% DMSO (vehicle, D) or with DMSO containing various concentrations of lapatinib (1.25, 2.5, 5, or 10 M) for 3 days. Relative amounts of viable cells were detected by MTS assay. O.D. values from DMSO-treated control cells were designated 100%. Lapatinib 按~100 mg/kg剂量口服处理,每天两次,显著抑制BT474和HN5移植瘤生长,这种作用存在剂量依赖性。[1] 与在体外活性一致,Lapatinib按100-150 mg/kg剂量处理携带H1975肿瘤的小鼠,延迟肿瘤生长。[3] 体外激酶实验: 通过测量抑制肽底物磷酸化的情况而获得抑制酶活性的IC50值。通过杆状病毒表达系统纯化EGFR 和 ErbB2的细胞外激酶域。在96孔圆底板上进行EGFR和ErbB2反应,终体积为45 μL。反应混合物含50 mM 4-吗啉丙磺酸(pH 7.5), 2 mM MnCl2, 10 μM ATP, 1 μCi [γ33P] ATP/每次反应, 50 μM 肽 A [生物素-(氨基)-EEEEYFELVAKKK-CONH2], 1 mM 二流苏糖醇,及 1 μL DMSO(含连续稀释的Lapatinib,起始浓度为10 μM)。加入指定纯化的 1型受体胞内域,开始反应。加入的酶量为为1 pmol/每组反应(20 nM)在23oC下反应10分钟,加入45 μL 0.5%溶于水的磷酸,终止反应。终止反应混合物(75 μL) 转移到磷酸纤维过滤板上。板过滤,然后使用200 μL 0.5% 磷酸冲洗3次。每孔加入闪烁剂(50 μL) , 在Packard Topcount上测量每组反应。通过10点剂量反应曲线获得IC50值。 Cell lines: HFF, MCF-7, T47D, A-431, HN5, BT474, N87, CaLu-3, HB4a, 和 HB4a c5.2 Concentrations: 溶于 DMSO,终浓度为~100 μM Incubation Time: 72小时 Method: 使用不同浓度Lapatinib处理细胞72小时。使用亚甲基蓝染色测定相对细胞数。使用Spectra酶标仪在620 nm 处测定吸光值。通过碘化丙啶染色和渗透BrdUrd的抗体检测,测量细胞死亡和细胞周期分析。(Only for Reference) 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献): 2% DMSO+40% PEG 300+5% Tween 80+53% ddH2O * 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。 第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方) 药物溶于 μL DMSO溶液(母液浓度 mg/mL,注:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck); 体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。 体内配方配制方法:取 μL DMSO母液,加入 μL Corn oil,混匀澄清。 注意:1. 首先保证母液是澄清的; 2. 一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。 本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为: 质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol) 摩尔浓度计算公式 *在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。 用本工具协助配置特定浓度的溶液,使用的计算公式为: 开始浓度 x 开始体积 = 最终浓度 x 最终体积 稀释公式 稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 ) 在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。. 连续稀释计算器方程NCT04608409 Recruiting Drug: Lapatinib and Paclitaxel Ovarian Cancer Frederick R. Ueland M.D.|University of Kentucky November 16 2020 Phase 1NCT03075995 Unknown status Other: hight-fat breakfast Breast Cancer Sun Yat-sen University April 12 2017 Not ApplicableNCT02338245 Completed Drug: ASLAN001|Drug: Lapatinib|Drug: Capecitabine Metastatic Breast Cancer Aslan Pharmaceuticals December 29 2014 Phase 2NCT02294786 Terminated Drug: Lapatinib|Drug: Capecitabine|Drug: Octreotide Cancer Novartis Pharmaceuticals|Novartis December 17 2014 Phase 2NCT02158507 Active not recruiting Drug: Combination of Veliparib + Lapatinib Metastatic Triple Negative Breast Cancer University of Alabama at Birmingham|Scariot Foundation|GlaxoSmithKline|AbbVie July 2014 Not Applicable 在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。 操作手册 问题 1: If I need to use S1028 for treating tumor-bearing mice with injection, how could I prepare the solution? S1028 Lapatinib Ditosylate can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 10 mg/ml as clear solution. EGFR(wt), IC50=0.5 nM; EGFR(L858R), IC50=0.4 nM; EGFR(L858R/T790M), IC50=10 nM; HER2, IC50=14 nM. Irreversible, mutant-selective EGFR inhibitor with Ki of 21.5 nM and 303.3 nM for EGFRL858R/T790M and EGFRWT, respectively. Erlotinib (OSI-774, CP358774, NSC 718781, Tarceva)是一种EGFR抑制剂,IC50 为 2 nM,对EGFR的敏感性比对人c-Src 或 v-Ab高1000多倍。Erlotinib可诱导自噬。 Bemcentinib (R428, BGB324)是一种Axl抑制剂,IC50为14 nM,作用于Axl比作用于Abl选择性高100倍以上。作用于Axl选择性也比作用于Mer和Tyro3(高50到100倍)及InsR, EGFR, HER2,和PDGFRβ(高100倍以上)高。 Pexidartinib (PLX3397)是一种口服有效的多靶点CSF-1R,Kit (c-Kit),和 FLT3受体酪氨酸激酶抑制剂,其IC50分别为20 nM, 10 nM 和 160 nM。Pexidartinib (PLX3397) 可以诱导细胞凋亡和坏死,并具有抗肿瘤活性。Phase 3。 AC480 (BMS-599626)是一种选择性的,高效效的HER1和HER2抑制剂,IC50分别为20 nM和30 nM。比对HER4效果强8倍左右,而比对VEGFR2, c-Kit, Lck, MET等的作用强100倍以上。Phase 1。 Features:BMS-599626是口服生物有效性的人表皮生长因子受体 (HER) 激酶HER1/HER2选择性抑制剂。 CP-724714是一种有效的,选择性HER2/ErbB2抑制剂,IC50为10 nM,无细胞试验中比作用于EGFR,InsR,IRG-1R,PDGFR,VEGFR2,Abl,Src,c-Met等选择性高640多倍。Phase 2。 Features:CP-724,714可用于治疗抗Trastuzumab的过量表达erbB2的肿瘤。 Neratinib (HKI-272)是一种高度选择性的HER2和EGFR抑制剂,在无细胞试验中IC50分别为59 nM 和 92 nM;微弱抑制KDR和Src,对Akt,CDK1/2/4,IKK-2,MK-2,PDK1,c-Raf和c-Met没有显著的抑制作用。Phase 3。 Sapitinib (AZD8931)是一种可逆的,ATP竞争性EGFR,ErbB2和ErbB3抑制剂,无细胞试验中IC50分别为4 nM,3 nM和4 nM,作用于NSCLC细胞比Gefitinib或Lapatinib更有效,作用于ErbB家族比作用于MNK1和Flt选择性强100倍。Phase 2。 Mubritinib (TAK 165)是一种有效的HER2/ErbB2抑制剂,在BT-474细胞中IC50为6 nM;而在BT-474细胞系中对EGFR,FGFR,PDGFR,JAK1,Src和Blk没有抑制作用。Phase 1。 Tyrphostin AG 879有效抑制HER2/ErbB2,IC50为1 μM,作用于ErbB2比作用于PDGFR和EGFR选择性高100到500倍。 Gefitinib (ZD1839)是一种EGFR抑制剂,作用于NR6wtEGFR和NR6W细胞中的Tyr1173、Tyr992、Tyr1173和Tyr992,IC50 分别为37 nM、37nM、26 nM和57 nM。Gefitinib 可通过阻滞PI3K/AKT/mTOR信号通路来促进肺癌细胞的自噬和细胞凋亡。 Features:Gefitinib是有效的EGFR酪氨酸激酶抑制剂。 Tags: 购买Lapatinib (GW-572016) Ditosylate | Lapatinib (GW-572016) Ditosylate供应商 | 采购Lapatinib (GW-572016) Ditosylate | Lapatinib (GW-572016) Ditosylate价格 | Lapatinib (GW-572016) Ditosylate生产 | 订购Lapatinib (GW-572016) Ditosylate | Lapatinib (GW-572016) Ditosylate代理商

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