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Lapatinib

Chemical Structure : Lapatinib

CAS No.: 231277-92-2

Lapatinib (GW572016, GW-572016)

货号: PC-45894Not For Human Use, Lab Use Only.

Lapatinib (GW572016) is a reversible, selective dual tyrosine kinase inhibitor of both EGFR and ErbB2 with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Lapatinib (GW572016) is a reversible, selective dual tyrosine kinase inhibitor of both EGFR and ErbB2 with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.
Lapatinib (GW572016) displays no significant activity against other kinases, including ErbB4, c-Src, and c-Raf1.
Lapatinib (GW572016) reduces tyrosine phosphorylation of EGFR and erbB2, and inhibits activation of Erk1/2 and AKT both in vitro and in vivo.
Lapatinib (GW572016) inhibits tumor xenograft growth of the HN5 and BT474 cells in a dose-responsive manner at 30 and 100 mg/kg; orally active.

物理化学性质&存储条件

分子量 581.0576
分子式 C29H26ClFN4O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 39 mg/mL

Chemical Name/SMILES

4-Quinazolinamine, N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-

参考文献

1. Xia W, et al. Oncogene. 2002 Sep 12;21(41):6255-63.

2. Rusnak DW, et al. Mol Cancer Ther. 2001 Dec;1(2):85-94.

3. Konecny GE, et al. Cancer Res. 2006 Feb 1;66(3):1630-9.

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