| 產(chǎn)品描述： | AZ-5104 is an active, demethylated metabolite of AZD 9291. AZ-5104 is an?EGFR?inhibitor with?IC50s of 1, 6, 1, 25 and 7 nM for?EGFRL858R/T790M,?EGFRL858R,?EGFRL861Q,?EGFR?and ErbB4, respectively. |
| 靶點(diǎn)： |
EGFRL858R/T790M:1 nM (IC50);EGFRL858R:1 nM (IC50);EGFRL861Q:6 nM (IC50);EGFR:25 nM (IC50);ErbB4:7 nM (IC50);EGFRExon 19 deletion/T790M;EGFR |
| 體外研究： |
AZ-5104 inhibits EGFR phosphorylation with IC50s of 2, 1, 2, 53, and 33 nM in H1975 (EGFRL858R/T790M), PC-9VanR (EGFRExon 19 deletion/T790M), PC-9 (EGFRExon 19 deletion), H2073 (WT), and LOVO (WT), respectively. AZ5104 exhibits a reduced selectivity margin against wild-type EGFR when compared to AZD9291. AZ5104 display minimal off-target activity against other non-HER family kinases, but has the potential to target both HER2 and HER4 kinase activity |
| 體內(nèi)研究： |
The metabolite, AZ5104 (5 mg/kg/day), is effective in shrinking tumors in both C/L858R and C/L+T mice |
| 參考文獻(xiàn)： |
1. Cross DA, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61. |
| 溶解性： |
soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.059 ml |
10.297 ml |
20.594 ml |
| 5 mM |
0.412 ml |
2.059 ml |
4.119 ml |
| 10 mM |
0.206 ml |
1.03 ml |
2.059 ml |
| 50 mM |
0.041 ml |
0.206 ml |
0.412 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