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Submit ReviewLapatinib is a potent and selective dual ErbB2 (HER-2) and EGFR inhibitor (IC50 values are 9.8 and 10.2 nM, respectively). Selective for EGFR and ErbB-2 versus other proliferative kinases. Inhibits proliferation in multiple cancer cell lines (average IC50 values <0.16 μM). Exhibits 100-fold average selectivity for the tumor cells versus human foreskin fibroblasts. Inhibits EGFR/ErbB2 autophosphorylation and phosphorylation of the downstream modulator AKT.
Lapatinib is also offered as part of the Tocriscreen Kinase Inhibitor Library and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
分子量 | 581.06 |
公式 | C29H26ClFN4O4S |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 231277-92-2 |
PubChem ID | 208908 |
InChI Key | BCFGMOOMADDAQU-UHFFFAOYSA-N |
Smiles | CS(=O)(CCNCC1=CC=C(C2=CC=C3N=CN=C(C3=C2)NC4=CC(Cl)=C(C=C4)OCC5=CC(F)=CC=C5)O1)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 58.11 | 100 |
以下数据基于产品分子量 581.06。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.72 mL | 8.6 mL | 17.21 mL |
5 mM | 0.34 mL | 1.72 mL | 3.44 mL |
10 mM | 0.17 mL | 0.86 mL | 1.72 mL |
50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
参考文献是支持产品生物活性的出版物。
Rusnak et al (2001) The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol.Cancer Ther. 1 85 PMID: 12467226
If you know of a relevant reference for Lapatinib, please let us know.
关键词: Lapatinib, Lapatinib supplier, Potent, selective, dual, ErbB2, (HER-2), and, EGFR, inhibitors, inhibits, 6811, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Lapatinib 的部分引用包括:
Gregory et al (2021) A ligand-receptor interactome platform for discovery of pain mechanisms and therapeutic targets. Sci Signal 14 PMID: 33727337
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