AZ-5104

Modify Date: 2024-01-09 22:48:59

AZ-5104 Structure
AZ-5104 structure
Common Name AZ-5104
CAS Number 1421373-98-9 Molecular Weight 485.581
Density 1.3±0.1 g/cm3 Boiling Point N/A
Molecular Formula C27H31N7O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of AZ-5104


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.

 Names

Name az5104
Synonym More Synonyms

 AZ-5104 Biological Activity

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.

 Chemical & Physical Properties

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

 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
Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: AZ5104
  • Price: $400.0/100mg $800.0/250mg $1600.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

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Price: $66/10mM*1mLinDMSO

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