2. JAK/STAT Signaling
    Stem Cell/Wnt
  3. STAT
  4. Homoharringtonine

Homoharringtonine (Synonyms: Omacetaxine mepesuccinate; HHT)

製品番号: HY-14944 純度: 99.96%
取扱説明書

Homoharringtonine (Omacetaxine mepesuccinate;HHT) is a cytotoxic alkaloid with antitumor properties which acts by inhibiting translation elongation.

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Homoharringtonine 構造式

Homoharringtonine 構造式

CAS 番号 : 26833-87-4

容量 価格（税別） 在庫状況 数量
10 mM * 1 mL in DMSO USD 112 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 102 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 348 在庫あり
Estimated Time of Arrival: December 31
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カスタマーレビュー

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Homoharringtonine purchased from MCE. Usage Cited in: Oncotarget. 2017 Jun 6;8(23):37594-37604.

    The expression of apoptosis proteins. K562/G01 cells treated with HHT 0, 50nM, 100 nM, 200nM for 24h. Bcl-2, caspase9, caspase3 express.

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    すべてのアイソフォームを表示
    STAT3 STAT5 STAT6

    • 生物活性

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    製品説明

    Homoharringtonine (Omacetaxine mepesuccinate;HHT) is a cytotoxic alkaloid with antitumor properties which acts by inhibiting translation elongation.

    IC50 & Target

    STAT3[1]
    体外実験

    Homoharringtonine inhibits IL-6-induced STAT3 phosphorylation in a dose- and time-dependent manner. Homoharringtonine (HHT) inhibits cells growth, cell viability and colony formation, as well as induced cell apoptosis through mitochondria pathway. The cytotoxicity of Homoharringtonine on human NSCLC cell lines is investigated, A549 (wild type EGFR) and NCI-H1975 (H1975, mutant EGFR with L858R and T790M), Gefitinib is used as a control. By MTT assay, Homoharringtonine has moderate cytotoxicity to A549 with an IC50 of 3.7 μM and H1975 cells are more sensitive to Homoharringtonine with an IC50 of 0.7 μM. Homoharringtonine inhibits the cell proliferation and growth of A549 cells and H1975 cells in a time- and dose-dependent manner through MTT assay. By trypan blue exclusion assay, Homoharringtonine rapidly reduces viable A549 and H1975 cells in a dose- and time-dependent manner. Homoharringtonine significantly inhibits the clonogenic ability of A549 and H1975 cells[1].
    体内実験

    Homoharringtonine (10 mg/kg) efficiently represses tumor growth compared to vehicle control or Gefitinib (P<0.05). Additionally, Homoharringtonine (HHT) treatment does not reduce the mice body weight, which suggests that Homoharringtonine has no apparent side effect. All the mice are euthanized, the tumors are isolated and imaged and the tumor sample cells are harvested to extract protein for determination if Homoharringtonine inhibits STAT3 phosphorylation via western blot. The level of STAT3 phosphorylation and MCL1 from Homoharringtonine treatment group is significantly decreased compared to vehicle control or Gefitinib treatment. Meanwhile, consistant with the results in the above, AKT1/2/3 and ERK1/2 phosphorylation is not inhibited with Homoharringtonine treatment. To further examine the STAT3 phosphorylation in the xenograft tumor samples with different treatments, the tumor samples are frozen and cutted into 10 μm sections for fluorescent immunohistochemistry. Homoharringtonine treatment inhibits STAT3 phosphorylation compared to vehicle control or Gefitinib treatment[1].
    臨床実験
    分子量

    545.62

    分子式

    C₂₉H₃₉NO₉
    CAS 番号

    26833-87-4
    SMILES

    [H][[email protected]@]12[[email protected]](CCC3)(C=C(OC)[[email protected]]2(OC([[email protected]](CCCC(O)(C)C)(O)CC(OC)=O)=O)[H])N3CCC4=CC5=C(OCO5)C=C14
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 50 mg/mL (91.64 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8328 mL 9.1639 mL 18.3278 mL
    5 mM 0.3666 mL 1.8328 mL 3.6656 mL
    10 mM 0.1833 mL 0.9164 mL 1.8328 mL
    *Please refer to the solubility information to select the appropriate solvent.
    体内:
    • 1.

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

      Solubility: ≥ 2.5 mg/mL (4.58 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (4.58 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (4.58 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    参考文献
    細胞実験
    [1]

    Human NSCLC cell lines MCF-10A, A549 and H1975 cells are seeded into 96-well plate and precultured for 24 h, then treated with Homoharringtonine for 24 h or 48 h. Cell cytotoxicity is determined by MTT assay. The absorbance is measured at 570 nm by Varioskan Flash Multimode Reader, and the cell death rate is calculated. Cell viability is estimated by trypan blue dye exclusion assay. The cells which exclude the dye are viable. Place 0.5 mL of a suitable cell suspension (dilute cells in complete medium without serum to 1×106 cells per mL) following adding 0.1 mL of 0.4% trypan blue dye and mixing thoroughly, and then incubate at room temperature for 3 min and load into a hemacytometer to count cells in three separate fields (nonviable, deep blue cells as well as viable, clear cells). The cell viability rate is calculated. After staining with Hoechst 33258 at 10 mg/mL for 10 min, cell death is observed by a fluorescence microscope[1].

    MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [1]

    Mice[1] Equal amounts of female and male nude immunodeficient mice (nu/nu), 6-8 weeks old, are injected subcutaneously with NSCLC H1975 cells (2.5×106) suspended in 100 μL RPMI-1640 medium into the rightflank of each mouse. Treatments are started when the tumors reached a palpablesize. Mice are randomly divided into three groups (n=10) and treated with Homoharringtonine (10 mg/kg), Gefitinib (30 mg/kg) or vehicle control for 3 weeks. Vernier caliper measurements of the longest perpendicular tumor diameters are conducted along with the mice treatment to estimate the tumor volume, using the following formula: 4π/3×(width/2)2×(length/2), representing the 3-dimensional volume of an ellipse tumor tissue. Animals are sacrificed when tumors reached to 2 cm or if the mice appeared moribund to prevent unnecessary morbidity to the mice. At the time of the animals’ death, tumors are excised; cells are separatedand lyzed for western blot using anti-STAT3 antibody, anti-pSTAT3, anti-MCL1 and anti-GAPDH antibodies and immunohistochemistry.

    MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    純度: 99.96%

    COA (143 KB) HNMR (265 KB) LCMS (116 KB)

    取扱説明書 (2659 KB)
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    Keywords:

    HomoharringtonineOmacetaxine mepesuccinateHHTSTATInhibitorinhibitorinhibit

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    製品番号:
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