| 產(chǎn)品描述： | Poziotinib(NOV120101; HM781-36B) is an irreversible HER1/2/4 inhibitor (IC50s: 3/5/23 nM). |
| 靶點(diǎn)： |
Apoptosis;EGFR;HER;Apoptosis;?EGFR;?HER |
| 體內(nèi)研究： |
Poziotinib對(duì)EGFR磷酸化和下游信號(hào)級(jí)聯(lián)放大的關(guān)鍵組分有抑制作用,如STAT3,AKT和ERK,且對(duì)HER2擴(kuò)增的胃癌細(xì)胞生長(zhǎng)有特異性抑制效果。經(jīng)激活HER2擴(kuò)增的胃癌細(xì)胞中線粒體途徑,Poziotinib還可誘導(dǎo)G1細(xì)胞周期阻滯和細(xì)胞凋亡。此外,在HER2誘發(fā)的和HER2非擴(kuò)增的胃癌細(xì)胞中,Poziotinib與化療劑有協(xié)同效果 |
| 細(xì)胞實(shí)驗(yàn)： |
Viable cell growth is determined by an MTT reduction assay. Briefly, all cell lines are seeded at a density of 3 × 103 per well in 96-well culture plates and then incubated at 37 °C for 24 h. The cells are then treated with 0.001, 0.01, 0.1, or 10 μM of HM781-36B. Three days later, 50 μg of MTT are added to each well and the samples are then incubated for 4 h to reduce the dye. Next, the samples are treated with DMSO, after which the absorbance of the converted dye in the living cells is measured at a wavelength of 540 nm. Six replicate wells are used for each analysis, and at least three independent experiments are conducted. Data points shown represent the mean while bars represent the SE.(Only for Reference) |
| 參考文獻(xiàn)： |
1.Nam HJ, et al. Cancer Lett. 2011, 302(2), 155-165. 2.Cha MY, et al. Int J Cancer. 2012, 130(10), 2445-2454. |
| 溶解性： |
H2O:<1 mg/mL DMSO:91 mg/mL (185.2 mM) Ethanol:<1 mg/mL |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.035 ml |
10.176 ml |
20.352 ml |
| 5 mM |
0.407 ml |
2.035 ml |
4.07 ml |
| 10 mM |
0.204 ml |
1.018 ml |
2.035 ml |
| 50 mM |
0.041 ml |
0.204 ml |
0.407 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。 |
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營(yíng)業(yè)執(zhí)照(三證合一)
北京