S81322 |
AZ-5104 |
| 源叶(MedMol) | 99% |
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- 产品描述： 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.
- 靶点： 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
- 体外研究： 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
- 体内研究： The metabolite, AZ5104 (5 mg/kg/day), is effective in shrinking tumors in both C/L858R and C/L+T mice
- 参考文献：
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
- 保存条件： -20℃
- 配置溶液浓度参考：
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
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