Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lapatinib ditosylate (Lapatinib tosilate) monohydrate 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 | ¥ 215 | 现货 | ||
25 mg | ¥ 345 | 现货 | ||
50 mg | ¥ 494 | 现货 | ||
100 mg | ¥ 654 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 323 | 现货 |
产品描述 | Lapatinib ditosylate (Lapatinib tosilate) monohydrate is a tyrosine kinase receptor inhibitor used in the therapy of advanced breast cancer and other solid tumors. Lapatinib ditosylate monohydrate therapy is associated with transient elevations in serum aminotransferase levels and rare instances of clinically apparent acute liver injury. |
靶点活性 | EGFR:10.8 nM, ErbB4:367 nM, ErbB2:9.2 nM |
激酶实验 | In vitro kinase assays: The IC50 values for inhibition of enzyme activity are generated by measuring 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. |
别名 | Lapatinib ditosylate monohydrate, Lapatinib ditoluenesulfonate monohydrate, Lapatinib tosilate hydrate, Lapatinib tosilate, Tykerb, 二甲苯磺酸拉帕替尼单水合物, Tyverb |
分子量 | 943.47 |
分子式 | C29H26ClFN4O4S·2(C7H8O3S)·H2O |
CAS No. | 388082-78-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 91 mg/mL(96.5 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.0599 mL | 5.2996 mL | 10.5992 mL | 26.4979 mL |
5 mM | 0.212 mL | 1.0599 mL | 2.1198 mL | 5.2996 mL | |
10 mM | 0.106 mL | 0.53 mL | 1.0599 mL | 2.6498 mL | |
20 mM | 0.053 mL | 0.265 mL | 0.53 mL | 1.3249 mL | |
50 mM | 0.0212 mL | 0.106 mL | 0.212 mL | 0.53 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 388082-78-8 Angiogenesis Apoptosis Autophagy JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR Ferroptosis HER1 Lapatinib ditosylate Monohydrate ErbB-1 Lapatinib ditosylate monohydrate GW2016 ditosylate Lapatinib Lapatinib ditoluenesulfonate monohydrate Lapatinib tosilate hydrate Lapatinib tosilate GW572016 ditosylate Lapatinib ditoluenesulfonate Monohydrate Lapatinib tosilate Hydrate Tykerb inhibit 二甲苯磺酸拉帕替尼单水合物 Lapatinib Ditosylate Tyverb Lapatinib ditoluenesulfonate Epidermal growth factor receptor Inhibitor inhibitor