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1421373-98-9

1421373-98-9 structure
1421373-98-9 structure
  • Name: AZ-5104
  • Chemical Name: az5104
  • CAS Number: 1421373-98-9
  • Molecular Formula: C27H31N7O2
  • Molecular Weight: 485.581
  • Catalog: Research Areas Cancer
  • Create Date: 2017-01-16 08:28:20
  • Modify Date: 2025-08-29 13:48:24
  • 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.

Name az5104
Synonyms metabolite of AZD9291
AZ 5104
Demethylated AZ9291
2-Propenamide, N-[2-[[2-(dimethylamino)ethyl]methylamino]-5-[[4-(1H-indol-3-yl)-2-pyrimidinyl]amino]-4-methoxyphenyl]-
AZ-5104
N-[2-[[2-(Dimethylamino)ethyl]methylamino]-5-[[4-(1H-indol-3-yl)-2-pyrimidinyl]amino]-4-methoxyphenyl]-2-propenamide
N-(5-((4-(1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide
N-(2-{[2-(Dimethylamino)ethyl](methyl)amino}-5-{[4-(1H-indol-3-yl)-2-pyrimidinyl]amino}-4-methoxyphenyl)acrylamide
Description 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.
Related Catalog
Target

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

In Vitro 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[1].
In Vivo The metabolite, AZ5104 (5 mg/kg/day), is effective in shrinking tumors in both C/L858R and C/L+T mice[1].
Cell Assay Cells were treated for 2 h with a dose-response of each drug (AZ-5104). Wild-type cells were stimulated for 10 minutes with 25 ng/mL of EGF before lysis. Level of EGFR phosphorylation was quantified in cell extracts using ELISA[1].
References

[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.

Density 1.3±0.1 g/cm3
Molecular Formula C27H31N7O2
Molecular Weight 485.581
Exact Mass 485.253937
PSA 98.41000
LogP 2.90
Index of Refraction 1.687
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