
Lapatinib是针对HER-1/ HER-2酪氨酸激酶抑制剂,继曲妥珠单抗(赫赛汀)后的第2个乳腺癌分子靶向新药,人ErbB受体属于I型受体酪氨酸激酶(TK)家族。包括ErbB1(EGFR)、ErbB2(HER2)、ErbB3(HER3)和ErbB4(HER4)。癌症患者ErbB-1(EGFR)和ErbB-2(HER-2)受体通常过度表达或发生其它改变。目前已知人类表皮生长因子受体-2(ErbB-2、HER-2)是目前认识较为清楚的与乳腺癌关系密切的人类癌基因,它在乳腺癌中的高表达往往预示着易有淋巴结转移和肿瘤分化差,预后不佳。随着对HER-2研究的深入,它已经成为乳腺癌特异性治疗的靶分子之一。Lapatinib是可逆的酪氨酸激酶抑制剂,能有效抑制ErbB1和ErbB2酪氨酸激酶活性。其作用的机理为抑制细胞内的EGFR(ErbB-1)和HER2(ErbB-2)的ATP位点阻止肿瘤细胞磷酸化和激活,通过EGFR(ErbB-1)和HER2(ErbB-1)的同质和异质二聚体阻断下调信号
Lapatinib is a promising new breast cancer medication. It is an oral therapy targeting intracellular components of a receptor known as ErbB2 and a second receptor, ErbB1, which have been implicated in the growth of various tumor types. Early tests have shown excellent results in treatment of breast cancer, and researchers hope to try Lapatinib on other solid tumor cancers.
Chemical Name: N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]-2-furyl] quinazolin-4-amine Bis(4-methylbenzenesulfonate) monohydrate
Appearance: Yellow crystalline powder.
CAS No.: [388082-78-8]
Identification: H-1 NMR spectrum-Conforms.
Melting Point: Min240℃ (decompose)
Water:1.5%-2.5%.
Assay (HPLC):Min98.5%
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