Cell Signaling Technology

Product Pathways - Tyrosine Kinase / Adaptors

Lapatinib #12121

EGFR   GW-572016   HER2   inhibitor  

Applications Dilution Species-Reactivity Sensitivity MW (kDa) Isotype

Species cross-reactivity is determined by western blot.

Applications Key:

Molecular Characterization






Chemical structure of lapatinib.拉帕替尼的化学结构。

Western Blotting

Western Blotting

Western blot analysis of extracts from SK-BR-3 cells, untreated or treated with Lapatinib (6 hr) at the indicated concentrations, using Phospho-HER2/ErbB2 (Tyr1248)/EGFR (Tyr1173) Antibody #2244 (upper) or HER2/ErbB2 (D8F12) XP® Rabbit mAb #4290 (lower).Western blot方法检测SK-BR-3细胞提取物,细胞未处理或用拉帕替尼在指定的浓度处理(6 hr),使用的抗体为Phospho-HER2/ErbB2 (Tyr1248)/EGFR (Tyr1173) Antibody #2244 (上图)或HER2/ErbB2 (D8F12) XP® Rabbit mAb #4290 (下图).

Directions for Use

Lapatinib is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 10 mg in 1.08 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but is typically used at 0.1-10 µM either as a pretreatment for 0.5-2 hr prior to treating with a stimulator or used alone with varying treatment times lasting up to 72 hr.

提供拉帕替尼的冻干粉末。将其10mg重新溶解在1.08 ml DMSO中,即为10 mM储存液。工作浓度和处理时间可以根据预期的效应而改变,但通常使用0.1-10 µM浓度在用刺激处理之前先预处理0.5-2 hr,或单独使用具有不同处理时间,最长达72小时。


Lapatinib is a dual inhibitor of EGFR and HER2 tyrosine kinases (1-4). Researchers have shown that lapatinib inhibits purified EGFR and HER2 tyrosine kinase domains in cell-free kinase assays with IC50 values of 10.8 nM and 9.2 nM, respectively, and HER4 with an IC50 of 367 nM. Lapatinib was greater than 300-fold more selective for HER2 and EGFR than many other kinases, including c-src, MEK, Erk, and p38 in these assays (1). Studies have shown that lapatinib effectively inhibits both EGFR and HER2 autophosphorylation in cell types over expressing these kinases, and cell growth inhibition is correlated with HER2 overexpression (2-4).

拉帕替尼是一种EGFR和HER2受体酪氨酸激酶的双重抑制剂(1-4)。研究表明,在无细胞激酶检测中,拉帕替尼抑制纯化的EGFR和HER2酪氨酸激酶结构域,IC50值分别为10.8 nM和9.2 nM,抑制HER4的IC50为367 nM。在这些检测分析中,拉帕替尼比许多其他激酶包括C-SRC,MEK,ERK和p38,对HER2和EGFR的选择性大300多倍(1)。有研究表明,在过表达这些激酶的细胞类型中,拉帕替尼有效地抑制EGFR和HER2受体的自身磷酸化,细胞生长抑制与HER2过表达有关(2-4)。

Application References

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For Research Use Only. Not For Use In Diagnostic Procedures.

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