Lapatinib

Lapatinib

参考价：¥500
供货周期： 一周
品牌：
规格： 2mg
货号： K1290
CAS号： 231277-92-2
上海高创化学科技有限公司
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SKU:K1290   M. Wt:581.06  
Formula:C29H26ClFN4O4S   Solubility:DMSO 100 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL  
Purity:>99%   Storage:2 years -20°C Powder  
CAS No.:231277-92-2   Synonyms:GW572016  
Chemical NameN-(4-(3-fluorobenzyloxy)-3-chlorophenyl)-6-(5-((2-(methylsulfonyl)ethylamino)methyl)furan-2-yl)quinazolin-4-amine,di4-methylbenzenesulfonate
Biological Activity
Description Lapatinib
Targets EGFR ErbB2      
IC50 10.8 nM 9.2 nM      
In vitro Lapatinib can inihbit Epidermal growth factor receptor (erbB1) with IC50 of 2.9 nM.[1] Lapatinib also inhibit receptor protein-tyrosine kinase(erbB-2) with IC50 around 3 nM.[1] Overexpression of ABC subfamily B member 1 (ABCB1) and ABC subfamily G member 2 (ABCG2) transporters would result in tumor multidrug resistance (MDR). Lapatinib significantly enhanced the sensitivity to ABCB1 or ABCG2 substrates in cells by stimulating the ATPase activity of both ABCB1 and ABCG2. And lapatinib reverses ABCB1- and ABCG2-mediated MDR by directly inhibiting their transport function so that lapatinib (Tykerb, GW572016) may combinate with other inhibitors to block proliferation of cancer cells and get better results. Lapatinib can inhibit SK-OV-3, an Ovarian carcinoma cell line which overexpress HER2, with IC50 from 3 to 4.5 nM.
In vivo N/A
Clinical Trials N/A
Features N/A

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