Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lapatinib Ditosylate (Tykerb ditosylate) 是一种有效的 EGFR 和 ErbB2 抑制剂,对 EGFR 和 ErbB2的 IC50值分别为 10.8 和 9.2 nM。它用于治疗晚期乳腺癌和其他实体瘤。
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) | ¥ 162 | 现货 |
产品描述 | Lapatinib Ditosylate (Tykerb ditosylate) is an effective EGFR and ErbB2 inhibitor (IC50: 10.8/9.2 nM for EGFR/ErbB2). |
靶点活性 | EGFR:10.8 nM (cell free), ErbB2:9.2 nM (cell free) |
体外活性 | Lapatinib (1 μM) induces apoptosis in NCI-N87 and OD19 cells [2]. Lapatinib inhibits the growth of EGFR-overexpressing A431 skin cancer (IC50: 0.14 μM) and ErbB2-overexpressing SK-BR-3 breast cancer cells (IC50: 0.124 μM). It also inhibits the growth of ErbB2-amplified OD19 esophageal (IC50: 0.09 μM)and NCI-N87 gastric cancer cells (IC50: 0.01 μM) as well as several types of gastric cancer cells in which ErbB2 is not amplified (IC50s: 0.35-8.58 μM) [3] . |
体内活性 | Lapatinib ( 30 and 100 mg/kg, p.o., b.i.d) dose-responsive inhibited the growth of BT474 and HN5 human tumor xenografts. Complete inhibition of tumor growth is seen at the 100 mg/kg dose. At this dose, there is <10% weight loss in treated animals over the course of the 21-day treatment. Lapatinib treatment inhibits tumor xenograft growth of the HN5 and BT474 cells in a dose-responsive manner at 30 and 100 mg/kg orally, twice daily, with complete inhibition of tumor growth at the higher dose [1]. Lapatinib (100 mg/kg/day, p.o.) induces severe oxidative damage in the cardiac tissue of rat [4]. |
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 | Lapatinib (GW-572016) Ditosylate, 二甲苯磺酸拉帕替尼, 二对甲苯磺酸拉帕替尼, GW-572016 ditosylate, Tykerb ditosylate |
分子量 | 925.46 |
分子式 | C29H26ClFN4O4S·2C7H8O3S |
CAS No. | 388082-77-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 93 mg/mL (100.5 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.0805 mL | 5.4027 mL | 10.8054 mL | 27.0136 mL |
5 mM | 0.2161 mL | 1.0805 mL | 2.1611 mL | 5.4027 mL | |
10 mM | 0.1081 mL | 0.5403 mL | 1.0805 mL | 2.7014 mL | |
20 mM | 0.054 mL | 0.2701 mL | 0.5403 mL | 1.3507 mL | |
50 mM | 0.0216 mL | 0.1081 mL | 0.2161 mL | 0.5403 mL | |
100 mM | 0.0108 mL | 0.054 mL | 0.1081 mL | 0.2701 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
Lapatinib Ditosylate 388082-77-7 Angiogenesis Apoptosis Autophagy JAK/STAT signaling Tyrosine Kinase/Adaptors Ferroptosis EGFR Inhibitor Lapatinib (GW-572016) Lapatinib (GW-572016) Ditosylate GW2016 ditosylate GW572016 ditosylate GW 572016 GW-572016 ErbB-1 inhibit HER1 Tykerb 二甲苯磺酸拉帕替尼 GW-572016 Ditosylate GW 572016 Ditosylate 二对甲苯磺酸拉帕替尼 Epidermal growth factor receptor GW572016 Tykerb Ditosylate GW-572016 ditosylate Lapatinib GW572016 Ditosylate Tykerb ditosylate inhibitor