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    AZ5104
    AZ5104

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0541
    CAS #: 1421373-98-9Purity ≥98%

    Description: AZ5104 (AZ-5104), a demethylated and active metabolite of Osimertinib (AZD-9291), is an irreversible EGFR inhibitor with potential antitumor activity. It inhibits EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4 with IC50s of 1, 6, 1, 25 and 7 nM, respectively. AZD9291 is a novel and selective third-generation irreversible inhibitor of both EGFRm(+) sensitizing and T790M resistance mutants that spares wild-type EGFR.

    References: Cancer Discov. 2014 Sep;4(9):1046-61.

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    AZ5104

    Name: AZ5104 (Osimertinib metabolite)
    CAS#: 1421373-98-9
    Chemical Formula: C27H31N7O2
    Exact Mass: 485.25392
    Molecular Weight: 485.58
    Elemental Analysis: C, 66.78; H, 6.43; N, 20.19; O, 6.59
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical Information

    Synonym: Demethylated AZ9291; active metabolite of AZD9291 (Osimertinib); AZ5104; AZ-5104; 

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

    InChi Key: IQNVEOMHJHBNHC-UHFFFAOYSA-N
    InChi Code: InChI=1S/C27H31N7O2/c1-6-26(35)30-22-15-23(25(36-5)16-24(22)34(4)14-13-33(2)3)32-27-28-12-11-21(31-27)19-17-29-20-10-8-7-9-18(19)20/h6-12,15-17,29H,1,13-14H2,2-5H3,(H,30,35)(H,28,31,32)
    SMILES Code: C=CC(NC1=CC(NC2=NC=CC(C3=CNC4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O.


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    In Vitro

    In vitro activity: AZ5104 shows great potency against ex19del (2 nM in PC-9), T790M (2 nM in H1975), and wild-type EGFR (33 nM in LOVO) cell lines. AZ5104 causes inhibition of cell viability with IC50 of 3.3 nM, 2.6 nM, 80 nM, and 53 nM for H1975 (T790M/L858R), PC-9 (ex19del), Calu 3 (WT), and NCI-H2073 (WT), respectively.


    Kinase Assay: Kinase assays are performed using peptide or protein substrates in a filter-binding radioactive ATP transferase assay for protein kinases, or lipid substrates and HTRF assay for lipid kinase.


    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

    In VivoIn both C/L858R and C/L+T mice, AZ5104 (5 mg/kg/d, p.o.) induces significant and sustained tumor regression.
    Animal modelMice bearing C/L858R and C/L+T tumors
    Formulation & Dosage Dissolved in 1% Polysorbate 80; 5 mg/kg; Oral gavage
    References

    Cancer Discov. 2014 Sep;4(9):1046-61.


    These protocols are for reference only. InvivoChem does not independently validate these methods.


     AZ5104


    AZD9291 binding mode and structure.  2014 Sep;4(9):1046-61.

     AZ5104


    Effect of AZD9291 on EGFR phosphorylation in vitro.  2014 Sep;4(9):1046-61.

     AZ5104


    In vivo anti-tumor efficacy of AZD9291 in subcutaneous xenograft models of EGFR-TKI sensitising and T790M resistant lung cancer.  2014 Sep;4(9):1046-61.

     AZ5104


    AZD9291 induces significant and sustained tumor regression in transgenic models of EGFR-TKI sensitising (C/L858R) and T790M resistant (C/L+T) lung cancer.  2014 Sep;4(9):1046-61.

     AZ5104


    AZD9291 inhibits EGFR phosphorylation and downstream signallng in murine models of EGFR T790M resistant lung cancer.   2014 Sep;4(9):1046-61.

     AZ5104


    Proof of concept clinical studies validating AZD9291 as a mutant-selective EGFR kinase T790M inhibitor.   2014 Sep;4(9):1046-61.


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