| 產(chǎn)品描述： | Icotinib Hydrochloride (BPI-2009) is a potent and specific?EGFR?inhibitor with an?IC50?of 5 nM; also inhibits mutant?EGFRL858R,?EGFRL858R/T790M,?EGFRT790M?and?EGFRL861Q |
| 靶點(diǎn)： |
EGFR:5 nM (IC50);EGFRL861Q;EGFRL858R/T790M;EGFRL858R;EGFRT790M ;EGFR |
| 體外研究： |
Incubation with Iconitib at 0.5 μM results in kinase activity inhibition of 91%, 99%, 96%, 61% and 61%, respectively. Iconitib inhibits the proliferation of A431 and BGC-823 A549, H460 and KB cell lines with IC50s of 1, 4.06, 12.16, 16.08, 40.71 μM. When profiled with 88 kinases, Icotinib only shows meaningful inhibitory activity to EGFR and its mutants. Icotinib blocks EGFR-mediated intracellular tyrosine phosphorylation (IC50=45 nM) in the human epidermoid carcinoma A431 cell line and inhibits tumor cell proliferation |
| 體內(nèi)研究： |
Icotinib exhibits potent dose-dependent antitumor effects in nude mice carrying a variety of human tumor-derived xenografts. The drug is well tolerated at doses up to 120 mg/kg/day in mice without mortality or significant body weight loss during the treatment. Icotinib inhibits tumor growth at a rate of 25.2%, 45.6% and 51.5% in the A431 cell line groups; 3.4%, 25.9% and 31.0% in the A549 cell line groups; 49.4%, 52.6% and 67.4% in the H460 cell line groups, and 30.3%, 36.4% and 46.5% in the HCT8 cell line groups, at 30, 60 and 120 mg/kg/dose, respectively |
| 參考文獻(xiàn)： |
1. Tan F, et al. Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies. Lung Cancer. 2012 May;76(2):177-82. |
| 溶解性： |
soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.337 ml |
11.685 ml |
23.371 ml |
| 5 mM |
0.467 ml |
2.337 ml |
4.674 ml |
| 10 mM |
0.234 ml |
1.169 ml |
2.337 ml |
| 50 mM |
0.047 ml |
0.234 ml |
0.467 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險(xiǎn)品化學(xué)品經(jīng)營(yíng)許可證（不帶存儲(chǔ)）
營(yíng)業(yè)執(zhí)照(三證合一)
北京