Homoharringtonine
(Synonyms: 高三尖杉酯碱; Omacetaxine mepesuccinate; HHT) 目录号 : GN10742
Homoharringtonine是一种蛋白质合成抑制剂和细胞毒性生物碱，最初从常绿树海南三尖杉中分离得到。Homoharringtonine常用于肺癌和乳腺癌的研究。
Cas No.:26833-87-4
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
Cell lines | A375 and B16F10 cells |
Preparation Method | The A375 and B16F10 cells were treated with different concentrations of Homoharringtonine (0-400nM) for 24 and 48h. |
Reaction Conditions | 0-400nM; 24-48h |
Applications | The colony formation, proliferation, and the cell cycle of A375 and B16F10 cells were inhibited obviously after treating with Homoharringtonine. |
| Animal experiment [2]: | |
Animal models | KrasG12D-expressing LL2 tumor modle |
Preparation Method | KrasG12D-expressing LL2 cells (2×105 cells in 200μl of PBS) were injected via the subcutaneous (s.c.) route into C57/BL6 mice. Tumor-bearing mice received intraperitoneal (i.p.) injections of Homoharringtonine (1.25-2.5 mg/kg) on day 10 after the tumor challenge, at two-day intervals, with a total of 10 i.p. injections administered. |
Dosage form | 1.25-2.5mg/kg; ip; two-day intervals, 20 days |
Applications | Homoharringtonine inhibited the growth of mouse lung tumor cells carrying Kras mutation in vivo, and decreased expression of endogenous ERK, STAT3, and Akt was observed in lung tumor cells. |
References:
[1]. Tang J, Li G, Zhang T, et al. Homoharringtonine inhibits melanoma cells proliferation in vitro and vivo by inducing DNA damage, apoptosis, and G2/M cell cycle arrest[J]. Archives of Biochemistry and Biophysics, 2021, 700: 108774.
[2]. Weng T Y, Wu H F, Li C Y, et al. Homoharringtonine induced immune alteration for an efficient anti-tumor response in mouse models of non-small cell lung adenocarcinoma expressing Kras mutation[J]. Scientific reports, 2018, 8(1): 8216
Homoharringtonine is a protein synthesis inhibitor and a cytotoxic alkaloid, originally isolated from the evergreen tree Cephalotaxus hainanensis. It is often used in the research of lung cancer and breast cancer[1].
Homoharringtonine (0-36.7nM; 0-96h) effectively inhibits the growth and viability of human acute myeloid leukemia cells and promotes cell cycle arrest, apoptosis and differentiation[1]. Homoharringtonine (0-400nM; 24-48h) inhibits the proliferation of melanoma cells A375 and B16F10 in vitro by inducing DNA damage, apoptosis, and G2/M cell cycle arrest[2]. Homoharringtonine (20nM; 0-48h) suppresses tumor proliferation and migration by regulating EphB4-mediated β-catenin loss in hepatocellular carcinoma[3].
In an A375 cell xenograft mice model, Homoharringtonine (1mg/kg; 10 days) can treat mice FLT3 mutant acute myeloid leukemia by targeting the SP1/TET1 pathway in acute myeloid leukemia cells and downregulating overall 5hmC levels[1]. Homoharringtonine (2.5mg/kg; two-day intervals; 20 days) inhibits the growth of lung tumor cells in mice carrying Kras mutations in vivo by altering cytokine expression in immune cells through inhibition of protein synthesis[4].
References：
[1]. Li C, Dong L, Su R, et al. Homoharringtonine exhibits potent anti-tumor effect and modulates DNA epigenome in acute myeloid leukemia by targeting SP1/TET1/5hmC[J]. haematologica, 2020, 105(1): 148.
[2]. Tang J, Li G, Zhang T, et al. Homoharringtonine inhibits melanoma cells proliferation in vitro and vivo by inducing DNA damage, apoptosis, and G2/M cell cycle arrest[J]. Archives of Biochemistry and Biophysics, 2021, 700: 108774.
[3]. Zhu, Man et al. “Homoharringtonine suppresses tumor proliferation and migration by regulating EphB4-mediated β-catenin loss in hepatocellular carcinoma.” Cell death & disease vol. 11,8 632. 14 Aug. 2020.
[4]. Weng T Y, Wu H F, Li C Y, et al. Homoharringtonine induced immune alteration for an efficient anti-tumor response in mouse models of non-small cell lung adenocarcinoma expressing Kras mutation[J]. Scientific reports, 2018, 8(1): 8216.
Homoharringtonine是一种蛋白质合成抑制剂和细胞毒性生物碱，最初从常绿树海南三尖杉中分离得到。Homoharringtonine常用于肺癌和乳腺癌的研究[1]。
Homoharringtonine（0-36.7nM；0-96h）可有效抑制人急性髓系白血病细胞的生长和活力，并促进细胞周期停滞、凋亡和分化[1]。Homoharringtonine（0-400nM；24-48h）通过诱导DNA损伤、凋亡和G2/M细胞周期停滞，抑制黑色素瘤细胞A375和B16F10体外增殖[2]。Homoharringtonine（20nM；0-48h）通过调节肝细胞癌中EphB4介导的β-catenin丢失来抑制肿瘤增殖和迁移[3]。
在A375细胞异种移植小鼠模型中，Homoharringtonine（1mg/kg；10 days) 可通过靶向急性髓系白血病细胞中的SP1/TET1通路并下调整体5hmC水平来治疗小鼠 FLT3 突变型急性髓系白血病[1]。Homoharringtonine（2.5mg/kg；两天间隔；20 days）可通过抑制蛋白质合成来改变免疫细胞中的细胞因子表达，从而抑制体内携带Kras突变的小鼠的肺肿瘤细胞生长[4]。
| Cas No. | 26833-87-4 | SDF | |
| 别名 | 高三尖杉酯碱; Omacetaxine mepesuccinate; HHT | ||
| 化学名 | (R)-1-((11bS,12S,14aR)-13-methoxy-2,3,5,6,11b,12-hexahydro-1H-[1,3]dioxolo[4',5':4,5]benzo[1,2-d]cyclopenta[b]pyrrolo[1,2-a]azepin-12-yl) 4-methyl 2-hydroxy-2-(4-hydroxy-4-methylpentyl)succinate | ||
| 分子式 | C29H39NO9 | 分子量 | 545.62 |
| 溶解度 | ≥ 181.2mg/mL in DMSO | 储存条件 | 4°C, protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。