AZ5104

This product is for research use only, not for human use. We do not sell to patients.

AZ5104
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Size Price Stock
250mg$750Check With Us
500mg$1250Check With Us
1g$1875Check With Us

Cat #: V0541 CAS #: 1421373-98-9 Purity ≥ 98%

Description: AZ5104 (AZ-5104), a demethylated and active metabolite of Osimertinib (AZD-9291), is an irreversible EGFR inhibitor with potential antitumor activity.

References: 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.

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Molecular Weight (MW)485.58
Molecular FormulaC27H31N7O2
CAS No.1421373-98-9
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
SMILES CodeC=CC(NC1=CC(NC2=NC=CC(C3=CNC4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O
SynonymsAZ5104; AZ-5104; AZ 5104. Demethylated AZ9291. metabolite of AZD9291;
ProtocolIn VitroAZ-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 VivoThe metabolite, AZ5104 (5 mg/kg/day), is effective in shrinking tumors in both C/L858R and C/L+T mice.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.0594 mL10.2970 mL20.5939 mL41.1879 mL
5mM0.4119 mL2.0594 mL4.1188 mL8.2376 mL
10mM0.2059 mL1.0297 mL2.0594 mL4.1188 mL
20mM0.1030 mL0.5148 mL1.0297 mL2.0594 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
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Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.