AZ5104( AZ5104 | AZ-5104 | AZ 5104. Demethylated AZ9291. metabolite of AZD9291 )

Catalog No. M11764 CAS No. 1421373-98-9

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

AZ5104
Note

Research use only, not for human use.
Brief Description

AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor.
Description

AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. Phase 1.
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.
In Vivo

The metabolite, AZ5104 (5 mg/kg/day), is effective in shrinking tumors in both C/L858R and C/L+T mice.
Synonyms

AZ5104 | AZ-5104 | AZ 5104. Demethylated AZ9291. metabolite of AZD9291
Pathway

Angiogenesis
Target

EGFR
Recptor

EGFR (L858R)| EGFR (L858R/T790M)| EGFR (L861Q)| EGFR (wildtype)| HER2/ErbB2
Research Area

Cancer
Indication

——

CAS Number

1421373-98-9
Formula Weight

485.58
Molecular Formula

C27H31N7O2
Purity

>98% (HPLC)
Solubility

Ethanol: 23 mg/mL warmed (47.36 mM); DMSO: 97 mg/mL (199.76 mM)
SMILES

C=CC(NC1=CC(NC2=NC=CC(C3=CNC4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O.
Chemical Name

N-(5-((4-(1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide

1. Cross DA, et al. Y Discov. 2014, 4(9), 1046-1061.

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