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Homoharringtonine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Homoharringtonine图片
CAS NO:26833-87-4
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
10mg电议
50mg电议
100mg电议
200mg电议

产品名称
高三尖杉酯碱
Omacetaxine mepesuccinate
HHT
产品介绍
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。
生物活性

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

IC50& Target

STAT3

 

体外研究
(In Vitro)

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 IC50of 3.7 μM and H1975 cells are more sensitive to Homoharringtonine with an IC50of 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].

体内研究
(In Vivo)

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].

Clinical Trial
分子量

545.62

性状

Solid

Formula

C29H39NO9

CAS 号

26833-87-4

中文名称

高三尖杉酯碱

结构分类
  • Alkaloids
  • Pyrrole Alkaloids
来源
  • Plants
  • Cephalotaxaceae
  • Cephalotaxus fortuneiHooker
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, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL(91.64 mM)

H2O : 1.4 mg/mL(2.57 mM;Need ultrasonic)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.8328 mL9.1639 mL18.3278 mL
5 mM0.3666 mL1.8328 mL3.6656 mL
10 mM0.1833 mL0.9164 mL1.8328 mL
*

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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

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

  • 1.

    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); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.58 mM,饱和度未知) 的澄清溶液。

    以 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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

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

    此方案可获得 ≥ 2.5 mg/mL (4.58 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

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

    此方案可获得 ≥ 2.5 mg/mL (4.58 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 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玉米油中,混合均匀。

  • 4.

    请依序添加每种溶剂: PBS

    Solubility: 1.67 mg/mL (3.06 mM); Clear solution; Need ultrasonic and warming and heat to 60℃

*以上所有助溶剂都可在本网站选购。