Lapatinib 拉帕替尼
货号：
IL0040
品牌：
Jinpan
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产品简介
| MDL | MFCD09264194 |
| EC | EINECS 1806241-263-5 |
| 别名 | GW572016; GSK572016 |
| CAS | 231277-92-2 |
| 分子式 | C29H26ClFN4O4S |
| 分子量 | 581.06 |
| 纯度 | ≥98% |
| 单位 | 瓶 |
| 生物活性 | Lapatinib (formerly GW572016, trade names Tykerb & Tyverb), usually used in the Ditosylate form, is a potent, orally bioavailable dual EGFR/ErbB2 inhibitor with potential anticancer activity. It inhibits epidermal growth factor receptor (EGFR)/ErbB2 with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. It is an FDA approved medication used for the treatment of breast cancer and other solid tumors. Lapatinib acts by reversibly blocking the phosphorylation of EGFR, ErbB2, and the Erk-1 and-2 and AKT kinases. [1] |
| In Vitro | Lapatinib (1 μM) induces apoptosis in NCI-N87 and OD19 cells [2]. Lapatinib inhibits the growth of EGFRoverexpressing 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] . |
| In Vivo | Lapatinib (100 mg/kg/day, p.o.) induces severe oxidative damage in the cardiac tissue of rat [4].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 [5]. |
| SMILES | O=S(CCNCC1=CC=C(C2=CC=C3C(C(NC4=CC(Cl)=C(C=C4)OCC5=CC(F)=CC=C5)=NC=N3)=C2)O1)(C)=O |
| 靶点 | EGFR |
| 数据来源文献 | [1]. Mol Cancer Ther. 2001 Dec;1(2):85-94; Cancer Res. 2006 Feb 1;66(3):1630-9. [2]. Chefrour M et al. Positive interaction between lapatinib and capecitabine in human breast cancer models: study of molecular determinants. Fundam Clin Pharmacol. 2012 Aug;26(4):530-7. [3]. Wainberg ZA, et al. Lapatinib, a dual EGFR and HER2 kinase inhibitor, selectively inhibits HER2-amplified human gastric cancer cells and is synergistic with trastuzumab in vitro and in vivo. Clin Cancer Res. 2010 Mar 1;16(5):1509-19. [4]. Eryilmaz U, et al. S100A1 as a Potential Diagnostic Biomarker for Assessing Cardiotoxicity and Implications for the Chemotherapy of Certain Cancers. PLoS One. 2015 Dec 18;10(12):e0145418. [5]. Rusnak DW, et al. 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. 2001 Dec;1(2):85-94 |
| 规格 | 5mg 10mM*1mL (in DMSO) 10mg |
是有效的 EGFR 和 ErbB2 抑制剂。