二甲苯磺酸拉帕替尼单水合物 T0078L

Product Introduction
Bioactivity


英文名: Lapatinib ditosylate monohydrate

描述: 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。

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.

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

溶解度: DMSO : 91 mg/mL(96.5 mM)


关键字: Lapatinib ditosylate | EGFR | HER1 | Lapatinib ditosylate Monohydrate | ErbB-1 | Ferroptosis | GW2016 ditosylate | Lapatinib | Autophagy | GW572016 ditosylate | Lapatinib ditoluenesulfonate Monohydrate | Lapatinib tosilate Hydrate | inhibit | Lapatinib Ditosylate | Lapatinib ditoluenesulfonate | Epidermal growth factor receptor | Inhibitor

相关产品: AG-494 | EGFR/CSC-IN-1 | Icotinib | Naquotinib mesylate | Mavelertinib | EGFR/ErbB-2/ErbB-4 inhibitor-2 | CP-724714 | Inetetamab | PROTAC EGFR degrader 8 | Desmethyl Erlotinib

相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途