AZ-5104
Modify Date: 2024-01-09 22:48:59
AZ-5104 structure
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Common Name | AZ-5104 | ||
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| 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-5104AZ-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 |
|---|---|
| Synonym | More Synonyms |
| 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. |
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| 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 |
| 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 |
| 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 |