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Homoharringtonine
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  • 货号 T3380
  • 品牌 TargetMol ( 经销商 )
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  • 规格/包装 10mg
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官网https://www.targetmol.cn/compound/homoharringtonine
产品编号 T3380别名 高三尖杉酯碱, Omacetaxine mepesuccinate, Myelostat, HHT, CeflatoninCas号 26833-87-4

Homoharringtonine (HHT) 属于生物碱类天然产物,可以抑制蛋白质的翻译,具有细胞毒性。Homoharringtonine 作用于肿瘤细胞的核糖体,抑制蛋白质翻译的延伸步骤,从而抑制蛋白质合成,具有抗肿瘤活性。


产品介绍

生物活性
产品描述
Homoharringtonine (HHT) is a natural alkaloid that inhibits the translation of proteins and is cytotoxic. Homoharringtonine acts on the ribosomes of tumor cells to inhibit the elongation step of protein translation, thereby inhibiting protein synthesis, and has antitumor activity.
体外活性
方法:人肺癌细胞 A549 和 NCI-H1975 用 Homoharringtonine (1-6 µM) 处理 24-48 h,使用 MTT assay 检测细胞活力。
结果:Homoharringtonine 对 A549 具有中等的细胞毒性,IC50 为 3.7  µM。H1975 细胞对 Homoharringtonine 更敏感,IC50 为 0.7  µM。[1]
方法:黑色素瘤细胞 A375 和 B16F10 用 Homoharringtonine (100 nM) 处理 48 h,使用 Flow cytometry 检测细胞周期和凋亡情况。
结果:Homoharringtonine 诱导 A375 和 B16F10 细胞凋亡和 G2/M 细胞周期停滞。[2]
体内活性
方法:为检测体内抗肿瘤活性,将 Homoharringtonine (10  mg/kg) 腹腔注射给携带人肺癌肿瘤 H1975 的 nude immunodeficient 小鼠,每周五次,持续三周。
结果:Homoharringtonine 能有效抑制肿瘤生长。Homoharringtonine 治疗组的 STAT3 磷酸化和 MCL1 水平显著降低。[1]
方法:为研究体内抗肿瘤活性,将 Homoharringtonine (0.7 mg/kg) 灌胃给药给携带 ccRCC 肿瘤移植物的 NOD/SCID 小鼠,每天两次,持续二十八天。
结果:两个肿瘤移植品系 XP26 和 XP144 在 Homoharringtonine 治疗后显示出可观察到的肿瘤生长抑制作用。对于 XP26 肿瘤,与载体处理的小鼠相比,Homoharringtonine 处理的小鼠的肿瘤生长被抑制 63.7%,而 XP144 小鼠的肿瘤增长被抑制 43.0%。[3]
细胞实验
Homoharringtonine (HHT) is dissolved in PBS at a stock solution of 2.5?mM and kept at ?20°C[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].
别名 高三尖杉酯碱, Omacetaxine mepesuccinate, Myelostat, HHT, Ceflatonin
化学信息
分子量 545.62
分子式 C29H39NO9
CAS No. 26833-87-4
Smiles COC(=O)CC(O)(CCCC(C)(C)O)C(=O)OC1C2c3cc4OCOc4cc3CCN3CCCC23C=C1OC
密度 1.33 g/cm3
储存&溶解度
存储 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 50 mg/mL (91.64 mM), Sonication is recommended. 
Chloroform, Dichloromethane, Ethyl Acetate, Acetone, etc.: Soluble
体内实验配方
5% DMSO+95% Saline: 4.55 mg/mL (8.34 mM), In vivo: Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. 
请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。
溶液配制表
DMSO
1mg 5mg 10mg 50mg
1 mM 1.8328 mL 9.1639 mL 18.3278 mL 91.6389 mL
5 mM 0.3666 mL 1.8328 mL 3.6656 mL 18.3278 mL
10 mM 0.1833 mL 0.9164 mL 1.8328 mL 9.1639 mL
20 mM 0.0916 mL 0.4582 mL 0.9164 mL 4.5819 mL
50 mM 0.0367 mL 0.1833 mL 0.3666 mL 1.8328 mL
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