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• 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。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *