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Cat. No.: HY-B0793GL

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AZ-5104 (GMP Like)

AZ-5104 (GMP-like) is the GMP-like grade of AZ-5104 (HY-B0793). 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 EGFR^L858R/T790M, EGFR^L858R, EGFR^L861Q, EGFR and ErbB4, respectively.

For research use only. We do not sell to patients.

CAS No.: 1421373-98-9
Formula: C₂₇H₃₁N₇O₂
Molecular Weight:485.58

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

AZ-5104 (GMP Like) Chemical Structure

CAS No.: 1421373-98-9

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Use of MCE Products

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
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Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

EGFR^L858R/T790M

1 nM (IC₅₀)

EGFR^L858R

1 nM (IC₅₀)

EGFR^L861Q

6 nM (IC₅₀)

EGFR

25 nM (IC₅₀)

ErbB4

7 nM (IC₅₀)

EGFR^{Exon 19 deletion/T790M}

All EGFR Isoforms :

In Vitro

AZ-5104 inhibits EGFR phosphorylation with IC₅₀s of 2, 1, 2, 53, and 33 nM in H1975 (EGFR^L858R/T790M), PC-9VanR (EGFR^{Exon 19 deletion/T790M}), PC-9 (EGFR^{Exon 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The metabolite, AZ5104 (5 mg/kg/day), is effective in shrinking tumors in both C/L858R and C/L+T mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 1421373-98-9
Molecular Weight 485.58
Formula C₂₇H₃₁N₇O₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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AZ-5104 (GMP Like)

All EGFR Isoforms