拉帕替尼(也稱為GW572016)是4-苯胺基喹唑啉類激酶抑制劑的一員，是表皮生長因子受體(EGFR)和人表皮生長因子受體2 (HER-2)酪氨酸激酶的有效、可逆和選擇性小分子抑制劑，在無細(xì)胞生化激酶試驗(yàn)中抑制重組EGFR和HER-2酪氨酸激酶，其50%抑制濃度IC50值分別為10.8 nmol/L和9.3 nmol/L。拉帕替尼干擾EGFR和HER-2的酪氨酸激酶結(jié)構(gòu)域中的三磷酸腺苷結(jié)合，導(dǎo)致抑制自身磷酸化和由此產(chǎn)生的下游信號(hào)活性(如細(xì)胞增殖和存活)。

產(chǎn)品性質(zhì)：

Cas No.：231277-92-2

別名：拉帕替尼; GW572016; GW2016

化學(xué)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

儲(chǔ)存條件：Store at -20°C

注意事項(xiàng)：

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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