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Lapatinib

Lapatinib

产品编号 T0078   CAS 231277-92-2
别名: GSK572016, GW572016, 拉帕替尼

Lapatinib (GW572016) 是一种 ErbB2 和 EGFR 的抑制剂 (IC50=9.2/10.8 nM),具有口服活性。Lapatinib 具有抗肿瘤活性,可以用于治疗 HER2 过表达的晚期或转移性乳腺癌。

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Lapatinib Chemical Structure
Lapatinib, CAS 231277-92-2
规格 价格/CNY 货期 数量
10 mg ¥ 197 现货
50 mg ¥ 583 现货
100 mg ¥ 996 现货
200 mg ¥ 1,460 现货
500 mg ¥ 2,515 现货
1 g ¥ 3,775 现货
1 mL * 10 mM (in DMSO) ¥ 244 现货
其他形式的 Lapatinib:
产品目录号及名称: Lapatinib (T0078)
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纯度: 99.89%
纯度: 99.68%
纯度: 99.03%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Lapatinib (GW572016) is an inhibitor of ErbB2 and EGFR (IC50=9.2/10.8 nM) with oral activity. Lapatinib has antitumor activity and can be used to treat advanced or metastatic breast cancer with HER2 overexpression.
靶点活性 EGFR:10.8 nM (cell free), ErbB2:9.2 nM (cell free)
体外活性 方法:14 株人胃癌和食管癌细胞系用 Lapatinib (0.3125-10 µmol/L) 处理 6 天,使用 particle counter 检测细胞数。
结果:N87、OE19、NUGC4、NUGC3、FU97、SNU16 细胞对 Lapatinib 敏感,IC50 分别为 0.01、0.09、0.35、2.24、4.86、8.58 μmol/L。[1]
方法:人乳腺癌细胞 MDA-MB-231 和 SK-BR-3 用 Lapatinib (0.5-2 µM) 处理 48 h,使用 Western Blot 方法检测靶点蛋白表达水平。
结果:与较低浓度相比,用 1.0 μM Lapatinib 处理的 MDA-MB-231 和 SK-BR-3 细胞系中 PKM2 的表达均显著降低。[2]
体内活性 方法:为检测体内抗肿瘤活性,将 Lapatinib (100 mg/kg) 腹腔注射给携带人胃癌肿瘤 N87 的 CD-1 athymic nude 小鼠,每天一次,持续三周。
结果:Lapatinib 导致 N87 异种移植物的肿瘤消退。[1]
方法:为检测体内抗肿瘤活性,将 Lapatinib (30-100 mg/kg,灌胃给药,每天两次持续二十一天) 和 Topoteca (6-10 mg/kg,腹腔注射,每四天一次持续三次) 灌胃给药给携带人乳腺癌肿瘤 BT474 的 SCID 小鼠。
结果:Lapatinib 和 Topoteca 组合在 ER2+BT474 异种移植物中显示出增强的功效。[3]
激酶实验 The IC50 values for inhibition of enzyme activity are generated by measuring the inhibition of phosphorylation of a peptide substrate. The intracellular kinase domains of EGFR and ErbB2 are purified from a baculovirus expression system. EGFR and ErbB2 reactions are performed in 96-well polystyrene round-bottomed plates in a final volume of 45 μL. Reaction mixtures contain 50 mM 4-morpholinepropanesulfonic acid (pH 7.5), 2 mM MnCl2, 10 μM ATP, 1 μCi of [γ33P] ATP/reaction, 50 μM Peptide A [Biotin-(amino hexonoic acid)-EEEEYFELVAKKK-CONH2], 1 mM dithiothreitol, and 1 μL of DMSO containing serial dilutions of Lapatinib beginning at 10 μM. The reaction is initiated by adding the indicated purified type-1 receptor intracellular domain. The amount of enzyme added is 1 pmol/reaction (20 nM). Reactions are terminated after 10 minutes at 23°C by adding 45 μL of 0.5% phosphoric acid in water. The terminated reaction mix (75 μL) is transferred to phosphocellulose filter plates. The plates are filtered and washed three times with 200 μL of 0.5% phosphoric acid. Scintillation cocktail (50 μL) is added to each well, and the assay is quantified by counting in a Packard Topcount. IC50 values are generated from 10-point dose-response curves [1].
细胞实验 Cells are plated in 96-well plates, in the media, at the following densities: HFF and HN5, 1000 cells/well and BT474, 5000 cells/well. After 24 h, the cells are exposed to vehicle (0.3% DMSO) or Lapatinib (1 nM, 10 nM, 100 nM, 1μM, 10μM, and 100μM). Lapatinib is removed from the cells after 72 h and is replaced by either DMEM containing 10% FBS and 50 μg/mL Gentamicin (HFF and HN5) or RPMI containing 10% FBS and 50 μg/mL Gentamicin (BT474). Methylene blue staining is performed at the time points over a total period of 16 days. Relative cell number is estimated using methylene blue staining. The absorbance at 620 nm is read in a Spectra microplate reader. Cell death and cell cycle analysis are assessed by propidium iodide staining and antibody detection of incorporated BrdUrd and staining with propidium iodide [1].
动物实验 CD-1 nude female mice are used for HN5 human tumor xenografts, which are initiated by injection of a cell suspension in PBS: Matrigel (1:1). C.B-17 SCID female mice are used for BT474 human tumor xenografts, which are initiated by implantation of tumor fragments (20-100 mg) from established tumors. Tumor cells and fragments are implanted by s.c. injection in the right flank. The s.c. tumors are measured with calipers, and mice are weighed twice weekly. Tumor weight is estimated from tumor volume using this formula: length×width2/2=tumor volume (mm3). Treatment begins when tumors are palpable, 3-5 mm in diameter. Lapatinib (30 and 100 mg/kg) is administered p.o. twice daily for 21 days in a vehicle of sulfo-butyl-ether-β-cyclodextrin 10% aqueous solution (CD10) [1].
别名 GSK572016, GW572016, 拉帕替尼
化合物与蛋白结合的复合物

T0078_1

crystal structure of the ErbB4 kinase in complex with lapatinib

分子量 581.06
分子式 C29H26ClFN4O4S
CAS No. 231277-92-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 93 mg/mL (160.1 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.721 mL 8.605 mL 17.2099 mL 43.0248 mL
5 mM 0.3442 mL 1.721 mL 3.442 mL 8.605 mL
10 mM 0.1721 mL 0.8605 mL 1.721 mL 4.3025 mL
20 mM 0.086 mL 0.4302 mL 0.8605 mL 2.1512 mL
50 mM 0.0344 mL 0.1721 mL 0.3442 mL 0.8605 mL
100 mM 0.0172 mL 0.086 mL 0.1721 mL 0.4302 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Wainberg ZA, et al. Lapatinib, a dual EGFR and HER2 kinase inhibitor, selectively inhibits HER2-amplified human gastric cancer cells and is synergistic with trastuzumab in vitro and in vivo. Clin Cancer Res. 2010 Mar 1;16(5):1509-19. 2. Guan M, et al. Lapatinib Inhibits Breast Cancer Cell Proliferation by Influencing PKM2 Expression. Technol Cancer Res Treat. 2018 Jan 1;17:1533034617749418. 3. Molina JR, et al. Evaluation of lapatinib and topotecan combination therapy: tissue culture, murine xenograft, and phase I clinical trial data. Clin Cancer Res. 2008 Dec 1;14(23):7900-8. 4. Eryilmaz U, et al. S100A1 as a Potential Diagnostic Biomarker for Assessing Cardiotoxicity and Implications for the Chemotherapy of Certain Cancers. PLoS One. 2015 Dec 18;10(12):e0145418.

文献引用

1. Pan Z, Wang K, Wang X, et al. Cholesterol promotes EGFR-TKIs resistance in NSCLC by inducing EGFR/Src/Erk/SP1 signaling-mediated ERRα re-expression. Molecular Cancer. 2022, 21(1): 1-17. 2. Kang J, Guo Z, Zhang H, et al. Dual Inhibition of EGFR and IGF-1R Signaling Leads to Enhanced Antitumor Efficacy against Esophageal Squamous Cancer. International Journal of Molecular Sciences. 2022, 23(18): 10382 3. Jiang L, Zeng Y, Ai L, et al. Decreased HMGB1 expression contributed to cutaneous toxicity caused by lapatinib. Biochemical Pharmacology. 2022: 115105 4. Zeng R, Yang X M, Li H W, et al.Simplified Derivatives of Tetrandrine as Potent and Specific P-gp Inhibitors to Reverse Multidrug Resistance in Cancer Chemotherapy.Journal of Medicinal Chemistry.2023 5. Sun R, Ge W, Zhu Y, et al.Proteomic Dynamics of Breast Cancer Cell Lines Identifies Potential Therapeutic Protein Targets.Molecular & Cellular Proteomics.2023: 100602.
Deferasirox Trigonelline PRLX-93936 HCL Trolox Artesunate Dopamine hydrochloride Imidazole ketone erastin (-)-Epicatechin

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌临床化合物库 酪氨酸激酶分子库 抗癌上市药物库 抗癌活性化合物库 HIF-1化合物库 临床期小分子药物库 抑制剂库 人代谢物化合物库 ReFRAME 相关化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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% ddH2O
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Lapatinib 231277-92-2 Angiogenesis Apoptosis Autophagy JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR Ferroptosis GW 572016 GW-2016 GSK-572016 GW 2016 HER1 Inhibitor ErbB-1 GSK572016 inhibit GW572016 拉帕替尼 GW-572016 GW2016 GSK 572016 Epidermal growth factor receptor inhibitor

 

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