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

Poziotinib (Synonyms: HM781-36B; NOV120101)

Cat. No.: HY-15730 Purity: 99.96%
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.

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Poziotinib Chemical Structure

Poziotinib Chemical Structure

CAS No. : 1092364-38-9

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10 mM * 1 mL in DMSO USD 106 In-stock
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5 mg USD 96 In-stock
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10 mg USD 132 In-stock
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50 mg USD 468 In-stock
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100 mg USD 708 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

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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 gefitinib or lapatinib[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].

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].

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: 99.96%

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KeyWords:

Poziotinib | HM781-36B | NOV120101 | NOV 120101 | NOV-120101 | EGFR | Apoptosis | Epidermal growth factor receptor | ErbB-1 | HER1 | Inhibitor | inhibitor | inhibit

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