拉帕替尼(也称为GW572016)是4-苯胺基喹唑啉类激酶抑制剂的一员，是表皮生长因子受体(EGFR)和人表皮生长因子受体2 (HER-2)酪氨酸激酶的有效、可逆和选择性小分子抑制剂，在无细胞生化激酶试验中抑制重组EGFR和HER-2酪氨酸激酶，其50%抑制浓度IC50值分别为10.8 nmol/L和9.3 nmol/L。拉帕替尼干扰EGFR和HER-2的酪氨酸激酶结构域中的三磷酸腺苷结合，导致抑制自身磷酸化和由此产生的下游信号活性(如细胞增殖和存活)。

产品性质：

Cas No.：231277-92-2

别名：拉帕替尼; GW572016; GW2016

化学名： N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine

Canonical SMILES CS(=O)(=O)CCNCC1=CC=C(O1)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl

分子式：C29H26ClFN4O4S

分子量：581.06

溶解度：≥ 29.05mg/mL in DMSO

储存条件：Store at -20°C

注意事项：

为了您的安全和健康，请穿实验服并戴一次性手套操作。

References:

[1].Alison Reid, Laura Vidal, Heather Shaw and Johann de Bono. Dual inhibition of ErbB1 (EGFR/HER1) and ErbB2 (HER2/neu). European Journal of Cancer 43 (2007) 481-489

[2].Norio Kondo, Mamoru Tsukuda, Yukari Ishiguro, Machiko Kimura, Kyoko Fujita, Atsuko Sakakibara, Hideaki Takahashi, Gabor Toth and Hideki Matsuda. Antitumor effects of lapatinib (GW572016), a dual inhibitor of EGFR and HER-2, in combination with cisplatin or paclitaxel on head and neck squamous cell carcinoma. Oncology Reports 23: 957-963, 2010

[3].Zev A. Wainberg, Adrian Anghel, Amrita J. Desai, Raul Ayala, Tong Luo, Brent Safran, Marlena S. Fejzo, J. Randolph Hecht, Denni J. Slamon and Richard S. Finn. 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; 16(5): 1509-1519