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

Osimertinib  (Synonyms: AZD-9291; Mereletinib)

Cat. No.: HY-15772 Purity: 99.92%
COA Handling Instructions

Osimertinib (AZD-9291) est un inhibiteur sélectif irréversible et mutant de EGFR avec des IC50s de 12 et 1 nM contre EGFRL858R et EGFRL858R/T790M, respectivement.

Osimertinib (AZD-9291) ist ein irreversibler und mutantenselektiver EGFR-Inhibitor mit IC50S-Werten von 12 und 1 nM gegen EGFRL858R bzw. EGFRL858R/T790M.

Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.

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

Osimertinib Chemical Structure

Osimertinib Chemical Structure

CAS No. : 1421373-65-0

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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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50 mg USD 100 In-stock
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200 mg USD 140 In-stock
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Customer Review

Based on 71 publication(s) in Google Scholar

Other Forms of Osimertinib:

Top Publications Citing Use of Products

60 Publications Citing Use of MCE Osimertinib

Proliferation Assay
WB

    Osimertinib purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219.   [Abstract]

    Measurement of antiproliferation effects of AZD9291 by EdU incorporation assay.

    Osimertinib purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219.   [Abstract]

    U87 and U251 cells are exposed to indicated concentrations of AZD9291 for 24 h and then stimulated with EGF (100 ng/mL) for 30 min. Cell lysates are prepared and examined using Western blot analysis with indicated antibodies.

    Osimertinib purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219.   [Abstract]

    U87 and U251 cells are treated with AZD9291 or CP-358774 for 4, 24 and 48 h. The expression level of p-ERK are assessed using Western blot analysis.

    Osimertinib purchased from MCE. Usage Cited in: Oncotarget. 2015 Oct 13;6(31):31313-22.  [Abstract]

    Effect of PCI-32765, WZ4002, AZD9291 and CO1686 on EGFR phosphorylation of tyrosines 1068 and 1173 in EGFR-dependent cancer cell lines.

    Osimertinib purchased from MCE. Usage Cited in: Cell Chem Biol. 2018 Aug 16;25(8):996-1005.e4.  [Abstract]

    Negligible increases in caspase-3 activity or PARP-1 cleavage is observed in H1975 NSCLC cells treated with DMSO, single agent PAC-1 (5 mM), or Osimertinib (Osi). In cells treated with PAC-1+Osimertinib, dramatic increases in caspase-3 activity is observed as early as 36 hr post treatment.

    Osimertinib purchased from MCE. Usage Cited in: Oncotarget. 2017 Mar 14;8(11):18359-18372.  [Abstract]

    In all of the cell lines tested, AZD9291 significantly affects the phosphorylation of eIF4E, which presumably is due to its strong inhibitory activity against MNK2 kinase.

    Osimertinib purchased from MCE. Usage Cited in: Oncotarget. 2017 Mar 14;8(11):18359-18372.  [Abstract]

    In all of the cell lines tested, AZD9291 significantly affects the phosphorylation of eIF4E, which presumably is due to its strong inhibitory activity against MNK2 kinase.

    Osimertinib purchased from MCE. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485.  [Abstract]

    Protein levels of p-EGFR(Tyr1068), p-EGFR(Tyr1137), EGFR, p-STAT3, STAT3, p-AKT, AKT, p-p38 MAPK, and p-ERK MAPK are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.

    Osimertinib purchased from MCE. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485.  [Abstract]

    Protein levels of p-EGFR(Tyr1068), p-EGFR(Tyr1137), EGFR, p-STAT3, STAT3, p-AKT, AKT, p-p38 MAPK, and p-ERK MAPK are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.

    Osimertinib purchased from MCE. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485.  [Abstract]

    Protein levels of NF-κB and IκB are analyzed are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.

    Osimertinib purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2019 Dec;40(12):1587-1595.  [Abstract]

    MDAMB-453 cells are pre-treated with 10 μM MG132 for 1 h before treatment with the 20 μM AZD for 4 h. Cell lysates were used for SDS PAGE and Western blotting. AZD9291 disrupts the EZH2–EED interaction by binding to EZH2 directly
    • Biological Activity

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    • Customer Review

    Description

    Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].

    IC50 & Target[1]

    EGFRL858R

    12 nM (IC50, Enzyme assays)

    EGFRL858R/T790M

    1 nM (IC50, Enzyme assays)

    In Vitro

    Osimertinib (AZD9291) (0-10 μM; 72 hours) dramatically inhibits cell proliferation with IC50s of 41, 26, 41, and 31 nM, respectively[2].
    Osimertinib (0-10 μM; 72 hours) inhibits cell proliferation (Ba/F3 cells harboring a T790M mutation, exon 19del+T790M, or L858R+T790M) with IC50s of 6, 7, and 74 nM, respectively[2].
    Osimertinib (0-10 μM; 72 hours) inhibits Ba/F3 cells harboring EGFR exon 20 insertion mutations (IC50 ranging from 16 to 701 nM for A763_Y764insFQEA (FQEA), Y764_V765insHH (HH), A767_V769dupASV (ASV), and D770_N771insNPG (NPG) cells)[2].
    Osimertinib shows high levels of phenotype potency in both sensitizing-mutant (mean IC50 of 8 nM in PC-9) and T790M (mean IC50s of 11 and 40 nM in H1975 and PC-9VanR respectively) EGFR cell lines. Osimertinib has much less activity towards wild-type EGFR (mean IC50s of 650 and 461 nM in Calu3 and H2073 respectively)[1].
    Osimertinib (0.1 μM; 48 hours) induces apoptosis in Ba/F3 cells (apoptosis rates of 40.9% and 90% in EGFR exon 19del+T790M, EGFR L858R+T790M respectively) [2].

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

    Cell Proliferation Assay[2]

    Cell Line: Ba/F3 cells (harboring a T790M mutation, exon 19del+T790M, or L858R+T790M)
    Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
    Incubation Time: 72 hours
    Result: Inhibited cell proliferation (IC50s=6, 7, 74 nM, respectively)

    Cell Proliferation Assay[2]

    Cell Line: PC-9, H3255, PC-9ER, and H1975 cells
    Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
    Incubation Time: 72 hours
    Result: Dramatically inhibited cell proliferation (IC50s=41, 26, 41, 31 nM, respectively)

    Cell Proliferation Assay[2]

    Cell Line: Ba/F3 cells (harboring EGFR exon 20 insertion mutations: FQEA, HH, ASV, NPG )
    Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
    Incubation Time: 72 hours
    Result: Inhibited cell proliferation (IC50s=16, 701, 230, 38 nM, respectively)

    Apoptosis Analysis[2]

    Cell Line: Ba/F3 cells (harboring EGFR exon 19del+T790M or EGFR L858R+T790M)
    Concentration: 0.1 μM
    Incubation Time: 48 hours
    Result: Induced apoptosis with the rates of 40.9% and 90% in EGFR T790M positive mutations cells, respectively.
    In Vivo

    Osimertinib (0.1-25 mg/kg; p.o.; daily for 14 days) induces significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models[1].

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

    Animal Model: PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models[1]
    Dosage: 0.1-10 mg/kg (PC-9 xenograft models); 0.5- 25 mg/kg (H1975 xenograft models)
    Administration: p.o.; daily for 14 days
    Result: Induced significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.
    Clinical Trial
    Molecular Weight

    499.61

    Formula

    C28H33N7O2

    CAS No.
    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 62.5 mg/mL (125.10 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0016 mL 10.0078 mL 20.0156 mL
    5 mM 0.4003 mL 2.0016 mL 4.0031 mL
    10 mM 0.2002 mL 1.0008 mL 2.0016 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  0.5%HPMC  1%Tween80

      Solubility: 5 mg/mL (10.01 mM); Suspened solution; Need ultrasonic and warming and heat to 60°C

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

    • 3.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

      Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

    • 4.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (4.16 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.92%

    References
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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