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

Poziotinib (Synonyms: HM781-36B; NOV120101)

Cat. No.: HY-15730 Purity: 99.97%
Handling Instructions

Poziotinib (HM781-36B) is an orally active, irreversible pan-HER inhibitor, which effectively inhibits EGFRwt, HER-2 and HER-4 with IC50s of 3.2, 5.3 and 23.5 nM, respectively. Poziotinib (HM781-36B) also shows excellent inhibitory activities against mutated EGFRs, including EGFRT790M and EGFRL858R/T790M, with IC50s of 4.2 and 2.2 nM, respectively. Excellent antitumor activity.

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

Poziotinib Chemical Structure

Poziotinib Chemical Structure

CAS No. : 1092364-38-9

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10 mg USD 132 In-stock
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100 mg USD 708 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Poziotinib purchased from MCE. Usage Cited in: Cancers (Basel). 2020 Nov 4;12(11):E3249.

    Poziotinib, at 0.1, 0.3 and 0.6 μM, produces a significant decrease in the expression level of the ABCG2 transporter protein in S1-M1-80 cells after 72 h of incubation, compared to cells incubated with vehicle (0 μM). ABCG2 protein expression is significantly decreased in S1-M1-80 cells following incubation with 0.6 µM of Poziotinib for 48 or 72 h.
    • Biological Activity

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    • Customer Review

    Description

    Poziotinib (HM781-36B) is an orally active, irreversible pan-HER inhibitor, which effectively inhibits EGFRwt, HER-2 and HER-4 with IC50s of 3.2, 5.3 and 23.5 nM, respectively. Poziotinib (HM781-36B) also shows excellent inhibitory activities against mutated EGFRs, including EGFRT790M and EGFRL858R/T790M, with IC50s of 4.2 and 2.2 nM, respectively. Excellent antitumor activity[1][2].

    IC50 & Target

    IC50: 3.2 nM (EGFRwt), 5.3 nM (HER-2), 23.5 nM (HER-4) 4.2 nM (EGFRT790M), 2.2 nM (EGFRL858R/T790M)[2]

    In Vitro

    The IC50 levels of Poziotinib (HM781-36B) for N87 and SNU216 were 0.001 and 0.004 μM, respectively, which was 10-1000 fold lower than the IC50 levels of other HER family TKIs. HM781-36B more potently inhibited the phosphorylation of HER family and downstream proteins, and induced apoptosis and G1 arrest compared to ZD1839 or GW572016[1].
    Poziotinib (HM781-36B) also shows excellent selectivity with other kinases with greater than 100- to 1,000- fold IC50 values compared with EGFR family members. Poziotinib (HM781-36B) possesses a functional α,β‐unsaturated carbonyl group as Michael acceptor moiety at the C6 position that allows covalent modifications of the EGFR kinase domain active site[2].
    The addition of HM781-36B induced potent growth inhibition in both DiFi cells with EGFR overexpression and SNU-175 cells (IC50=0.003 and 0.005 μM, respectively). Furthermore, HM781-36B induced G1 arrest of the cell cycle and apoptosis, and reduced the levels of HER family and downstream signaling molecules, pERK and pAKT, as well as nonreceptor/cytoplasmic tyrosine kinase, BMX[3].

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

    In Vivo

    The growth of tumors in mice treated with HM781-36B alone or in combination with 5-FU was significantly inhibited compared with control mice, and tumor volume in mice receiving coadministraion of HM781-36B and 5-FU was smaller than tumor volume in mice receiving HM781-36B only[1].

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

    Clinical Trial
    Molecular Weight

    491.34

    Formula

    C₂₃H₂₁Cl₂FN₄O₃

    CAS No.

    1092364-38-9

    SMILES

    C=CC(N1CCC(OC2=CC3=C(NC4=CC=C(Cl)C(Cl)=C4F)N=CN=C3C=C2OC)CC1)=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 : 135 mg/mL (274.76 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0353 mL 10.1763 mL 20.3525 mL
    5 mM 0.4071 mL 2.0353 mL 4.0705 mL
    10 mM 0.2035 mL 1.0176 mL 2.0353 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.25 mg/mL (4.58 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.25 mg/mL (4.58 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.97%

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    Keywords:

    PoziotinibHM781-36B NOV120101NOV120101NOV 120101NOV-120101EGFRApoptosisEpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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