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

Homoharringtonine  (Synonyms: 高三尖杉酯碱; Omacetaxine mepesuccinate; HHT)

目录号: HY-14944 纯度: 99.75%
COA 产品使用指南

Homoharringtonine (Omacetaxine mepesuccinate;HHT) 是具有抗肿瘤特性的细胞毒性生物碱,其通过抑制翻译延长来起作用。

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Homoharringtonine Chemical Structure

Homoharringtonine Chemical Structure

CAS No. : 26833-87-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥840
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5 mg ¥700
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10 mg ¥865
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50 mg ¥2400
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Customer Review

Other Forms of Homoharringtonine:

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

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

    查看 STAT 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

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

    IC50 & Target[1]

    STAT3

     

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    4T1 IC50
    0.06 μM
    Compound: 1; HHT
    Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    A204 IC50
    0.004 μM
    Compound: 1; HHT
    Antiproliferative activity against human A204 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human A204 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    A549 IC50
    0.03 μM
    Compound: Homoharringtonine
    Cytotoxicity against human A549 cells assessed as reduction of cell growth by SRB method
    Cytotoxicity against human A549 cells assessed as reduction of cell growth by SRB method
    [PMID: 18782668]
    A549 IC50
    18.28 nM
    Compound: HHT
    Inhibition of Nuclear factor erythroid 2-related factor 2 5'-untranslated region guanine-rich DNA sequence in human A549 cells harboring ARE-GFP-Luc assessed as reduction in ARE-luciferase activity after 24 hrs by firefly luciferase reporter gene assay
    Inhibition of Nuclear factor erythroid 2-related factor 2 5'-untranslated region guanine-rich DNA sequence in human A549 cells harboring ARE-GFP-Luc assessed as reduction in ARE-luciferase activity after 24 hrs by firefly luciferase reporter gene assay
    [PMID: 31270017]
    A549 IC50
    31.6 nM
    Compound: homoharringtonine
    Cytotoxicity against human A549 cells after 48 hrs by MTT assay
    Cytotoxicity against human A549 cells after 48 hrs by MTT assay
    [PMID: 31916761]
    BaF3 IC50
    0.081 μM
    Compound: 1; HHT
    Antiproliferative activity against mouse BaF3 cells expressing Bcr/Abl-T315I mutant assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against mouse BaF3 cells expressing Bcr/Abl-T315I mutant assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    Caco-2 CC50
    1.72 μM
    Compound: HOMOHARRINGTONINE
    Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
    Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
    10.21203/rs.3.rs-23951/v1
    Caco-2 IC50
    4.71 μM
    Compound: HOMOHARRINGTONINE
    Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
    Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
    10.21203/rs.3.rs-23951/v1
    HCT-116 IC50
    0.013 μM
    Compound: 1; HHT
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    HeLa IC50
    0.4 μM
    Compound: Homoharringtonine
    Cytotoxicity against human HeLa cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
    Cytotoxicity against human HeLa cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
    [PMID: 33905250]
    HeLa IC50
    1.7 μM
    Compound: HHT
    Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 68 hrs by MTS assay
    Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 68 hrs by MTS assay
    [PMID: 35148094]
    HepG2 IC50
    34.5 nM
    Compound: homoharringtonine
    Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
    Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
    [PMID: 31916761]
    HL-60 IC50
    0.013 μM
    Compound: 1; HHT
    Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    HL-60 IC50
    0.02 μM
    Compound: homoharringtonine
    Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by Alamar Blue assay
    Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by Alamar Blue assay
    10.1039/C0MD00241K
    HL-60 IC50
    0.022 μM
    Compound: HHT
    Antiproliferative activity against human HL60 cells after 62 hrs by MTS assay
    Antiproliferative activity against human HL60 cells after 62 hrs by MTS assay
    [PMID: 29286665]
    HL-60 IC50
    21.8 nM
    Compound: HHT
    Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth measured after 68 hrs by MTS assay
    Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth measured after 68 hrs by MTS assay
    [PMID: 35148094]
    Huh-7 IC50
    0.04 μM
    Compound: 1; HHT
    Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    K562 IC50
    0.014 μM
    Compound: 1; HHT
    Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    KB IC50
    0.004 μM
    Compound: Homoharringtonine
    Cytotoxicity against human KB cells assessed as reduction of cell growth by SRB method
    Cytotoxicity against human KB cells assessed as reduction of cell growth by SRB method
    [PMID: 18782668]
    L02 IC50
    0.064 μM
    Compound: 1; HHT
    Cytotoxicity against human HL7702 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Cytotoxicity against human HL7702 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    MDA-MB-453 IC50
    0.021 μM
    Compound: 1; HHT
    Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    MOLT-4 IC50
    0.007 μM
    Compound: 1; HHT
    Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    MV4-11 IC50
    0.005 μM
    Compound: 1; HHT
    Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    NCI-H1299 IC50
    0.022 μM
    Compound: 1; HHT
    Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    NCI-H1975 IC50
    0.022 μM
    Compound: 1; HHT
    Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    NCI-H716 IC50
    0.065 μM
    Compound: 1; HHT
    Antiproliferative activity against human NCI-H716 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human NCI-H716 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    OCI-Ly3 IC50
    0.005 μM
    Compound: 1; HHT
    Antiproliferative activity against human OCILY3 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human OCILY3 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    U-937 IC50
    0.012 μM
    Compound: 1; HHT
    Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    体外研究
    (In Vitro)

    Homoharringtonine 以剂量和时间依赖性方式抑制 IL-6 诱导的 STAT3 磷酸化。Homoharringtonine (HHT) 抑制细胞生长、细胞活力和集落形成,并通过线粒体途径诱导细胞凋亡。研究了 Homoharringtonine 对人 NSCLC 细胞系的细胞毒性,A549 (野生型 EGFR) 和 NCI-H1975 (H1975,具有 L858R 和 T790M 的突变型 EGFR),吉非替尼用作对照。MTT 法检测,Homoharringtonine 对 A549 具有中度细胞毒性,IC50 为 3.7 μM,H1975 细胞对 Homoharringtonine 更敏感,IC50 为 0.7 μM。通过 MTT 测定,Homoharringtonine 以时间和剂量依赖性方式抑制 A549 细胞和 H1975 细胞的细胞增殖和生长。通过台盼蓝排斥试验,Homoharringtonine 以剂量和时间依赖的方式快速减少活的 A549 和 H1975 细胞。Homoharringtonine 显著抑制 A549 和 H1975 细胞的克隆形成能力[1]

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

    体内研究
    (In Vivo)

    与载体对照或吉非替尼相比,Homoharringtonine (10 mg/kg) 可有效抑制肿瘤生长 (P<0.05)。此外,Homoharringtonine (HHT) 处理不会减轻小鼠体重,这表明 Homoharringtonine 没有明显的副作用。对所有小鼠实施安乐死,分离肿瘤并成像,收集肿瘤样本细胞以提取蛋白质,以通过蛋白质印迹确定 Homoharringtonine 是否抑制 STAT3 磷酸化。与载体对照或吉非替尼处理相比,Homoharringtonine 处理组的 STAT3 磷酸化和 MCL1 水平显著降低。同时,与上述结果一致,AKT1/2/3 和 ERK1/2 磷酸化未被 Homoharringtonine 处理抑制。为了进一步检查经过不同处理的异种移植肿瘤样本中的 STAT3 磷酸化,将肿瘤样本冷冻并切成 10 μM 的切片用于荧光免疫组织化学。与媒介物对照或吉非替尼处理相比,Homoharringtonine 处理抑制 STAT3 磷酸化[1]

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

    Clinical Trial
    分子量

    545.62

    Formula

    C29H39NO9

    CAS 号
    性状

    固体

    颜色

    Off-white to yellow

    中文名称

    高三尖杉酯碱

    结构分类
    初始来源
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, protect from light

    *In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : ≥ 50 mg/mL (91.64 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    H2O 中的溶解度 : 1.4 mg/mL (2.57 mM; 超声助溶)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 1 year; -20°C, 6 months (protect from light)。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.58 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.58 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

    以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂: PBS

      Solubility: 1.67 mg/mL (3.06 mM); 澄清溶液; 超声助溶 (<60°C)

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

    *In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.96%

    参考文献
    Cell Assay
    [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 has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [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 has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 1 year; -20°C, 6 months (protect from light)。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 1.8328 mL 9.1639 mL 18.3278 mL 45.8194 mL
    DMSO 5 mM 0.3666 mL 1.8328 mL 3.6656 mL 9.1639 mL
    10 mM 0.1833 mL 0.9164 mL 1.8328 mL 4.5819 mL
    15 mM 0.1222 mL 0.6109 mL 1.2219 mL 3.0546 mL
    20 mM 0.0916 mL 0.4582 mL 0.9164 mL 2.2910 mL
    25 mM 0.0733 mL 0.3666 mL 0.7331 mL 1.8328 mL
    30 mM 0.0611 mL 0.3055 mL 0.6109 mL 1.5273 mL
    40 mM 0.0458 mL 0.2291 mL 0.4582 mL 1.1455 mL
    50 mM 0.0367 mL 0.1833 mL 0.3666 mL 0.9164 mL
    60 mM 0.0305 mL 0.1527 mL 0.3055 mL 0.7637 mL
    80 mM 0.0229 mL 0.1145 mL 0.2291 mL 0.5727 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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      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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    产品名称:
    Homoharringtonine
    目录号:
    HY-14944
    需求量: