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    Osimertinib (AZD9291; Tagrisso)
    Osimertinib (AZD9291; Tagrisso)

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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 #: V0546
    CAS #: 1421373-65-0Purity ≥98%

    Description: Osimertinib (formerly AZD-9291 and mereletinib; trade name Tagrisso) is an oral bioavailable, irreversible/covalent, and mutant-selective EGFR inhibitor with potential antineoplastic activity. It inhibits Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells with IC50s of 12.92, 11.44 and 493.8 nM, respectively. It was approved in 2017 by both FDA and the European Commission for cancer treatment.

    References: Transl Lung Cancer Res. 2014 Dec;3(6):370-2; J Med Chem. 2014 Oct 23;57(20):8249-67. 

    Related CAS: 1421372-66-8(AZD9291 DA - the des acryl derivative of AZD9291); 1421373-66-1 (mesylate); 1421373-65-0 (free base) 

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    • 香港大学
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    Molecular Weight (MW)499.61
    FormulaC28H33N7O2
    CAS No.1421373-65-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 99 mg/mL (198.12 mM)
    Water: <1 mg/mL
    Ethanol: 43 mg/mL (86.01 mM)
    Solubility (In vivo)1% DMSO+30% PEG 300+dd H2O: 30mg/mL
    SynonymsAZD-9291;  AZD9291; AZD 9291; Osimertinib free base; Mereletinib; Trade name: Tagrisso 

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

    InChi Key: DUYJMQONPNNFPI-UHFFFAOYSA-N

    InChi Code: InChI=1S/C28H33N7O2/c1-7-27(36)30-22-16-23(26(37-6)17-25(22)34(4)15-14-33(2)3)32-28-29-13-12-21(31-28)20-18-35(5)24-11-9-8-10-19(20)24/h7-13,16-18H,1,14-15H2,2-6H3,(H,30,36)(H,29,31,32)

    SMILES Code: C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O


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    In Vitro

    In vitro activity: AZD9291 shows significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro.


    Kinase Assay: Osimertinib (formerly known as AZD-9291 and mereletinib) is an oral available, irreversible, and mutant-selective, 3rd generation EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. It inhibits both activating and resistant EGFR mutations while sparing the normal form of EGFR that is present in normal skin and gut cells, thereby reducing the side effects encountered with currently available medicines.


    Cell Assay: AZD9291 potently inhibits EGFR phosphorylation in EGFRm+ (e.g. PC9; < 25 nM) and EGFR m+/T790M (e.g. H1975; < 25 nM) cell lines in vitro, whilst demonstrating much less activity against wild-type EGFR lines (e.g. LoVo; > 500 nM). Consistently, AZD9291 showed significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro.

    In VivoAZD9291(5mg/kg p.o.) causes profound regression of tumors across EGFRm+ (PC9) and EGFRm+/T790M (H1975) tumor models with profound inhibition of EGFR phosphorylation and key downstream signaling pathways such as AKT and ERK in vivo.
    Animal modelEGFRm+ and EGFRm+/T790M transgenic mice
    Formulation & Dosage5 mg/kg; p.o
    ReferencesTransl Lung Cancer Res. 2014 Dec;3(6):370-2; J Med Chem. 2014 Oct 23;57(20):8249-67. 


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

    Osimertinib (AZD9291)

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

    Osimertinib (AZD9291)

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

    Osimertinib (AZD9291)

    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.

    Osimertinib (AZD9291)

    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.

    Osimertinib (AZD9291)

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

    Osimertinib (AZD9291)

    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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