拉帕替尼
| CAS号 | 231277-92-2 | 货号 | BCP01874 |
| 中文名 | 拉帕替尼 | ||
| 英文名 | Lapatinib | ||
| 中文别名 | |||
| 英文别名 | GSK572016; GSK-572016; GSK 572016; GW2016; GW-2016; GW 2016; | ||
| 分子式 | C29H26ClFN4O4S | 分子量 | 581.06 |
| 生物活性 | Lapatinib weakly inhibits the activity of ErbB4 with IC50 of 367 nM, and displays >300-fold selectivity for EGFR and ErbB2 over other kinases such as c-Src, c-Raf, MEK, ERK, c-Fms, CDK1, CDK2, p38, Tie-2, and VEGFR2. Lapatinib significantly inhibits receptor autophosphorylation of EGFR and ErbB2 in a dose-dependent manner with IC50 of 170 nM and 80 nM, respectively in HN5 cells; as well as 210 nM and 60 nM, respectively in BT474 cells. Unlike OSI-774 and Iressa (ZD1839) which preferentially inhibit the growth of the EGFR-overexpressing cells, Lapatinib inhibits the growth of both EGFR- and ErbB2-overexpressing cells. | ||
| 上下游产品 | 388082-78-8（二甲苯磺酸拉帕替尼） 388082-77-7（二对甲苯磺酸拉帕替尼） | ||
| 信号通路 | Angiogenesis/Protein Tyrosine Kinase Jak/Stat Pathway | ||
| 靶 点 | EGFR HER2 | ||
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Molecular regulation of apoptotic machinery and lipid metabolism by mTORC1/mTORC2 dual inhibitors in preclinical models of HER2+/PIK3CAmut breast cancer
购于瀚香生物(Biochempartner)的拉帕替尼(CAS:231277-92-2)被引用 |
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mTOR complex-2 stimulates acetyl-CoA and de novo lipogenesis through ATP citrate lyase in HER2/PIK3CA-hyperactive breast cancer
购于瀚香生物(Biochempartner)的拉帕替尼(CAS:231277-92-2)被引用 |
结构式
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