1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR

AZ-5104 

Cat. No.: HY-B0793 Purity: 99.97%
Data Sheet SDS Handling Instructions

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.

For research use only. We do not sell to patients.
AZ-5104 Chemical Structure

AZ-5104 Chemical Structure

CAS No. : 1421373-98-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 66 In-stock
5 mg USD 60 In-stock
10 mg USD 108 In-stock
50 mg USD 384 In-stock
100 mg USD 624 In-stock
200 mg USD 864 In-stock
500 mg   Get quote  
1 g   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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.

IC50 & Target

IC50: 1 nM (EGFRL858R/T790M), 6 nM (EGFRL858R),1 nM EGFRL861Q,1 nM (EGFR),1 nM (ErbB4)[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[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].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.0594 mL 10.2970 mL 20.5939 mL
5 mM 0.4119 mL 2.0594 mL 4.1188 mL
10 mM 0.2059 mL 1.0297 mL 2.0594 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

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

References
Molecular Weight

485.58

Formula

C₂₇H₃₁N₇O₂

CAS No.

1421373-98-9

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 28 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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AZ-5104
Cat. No.:
HY-B0793
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