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Purity: ≥98%
Homoharringtonine (Omacetaxine mepesuccinate and HHT; trade name Synribo) is a naturally occurring and cytotoxic pharmaceutical substance that is indicated for treatment of chronic myeloid leukemia (CML). It acts by inhibiting translation elongation. It is a natural product first discovered in Cephalotaxus harringtonia, now manufactured by hemi-synthesis. It was approved by the US FDA in October 2012 for the treatment of adult patients with CML with resistance and/or intolerance to two or more tyrosine kinase inhibitors (TKIs).
| ln Vitro |
Homoharringtonine exhibits antagonistic effects on both dose and time in inhibiting IL-6-induced STAT3 phosphorylation. Through mechanisms, homoharringtonine (HHT) causes apoptosis while suppressing colony formation, cell proliferation, and survival. Homoharringtonine's cytotoxicity was investigated using gefitinib-controlled human non-small cell lung cancer (NSCLC) cell lines, A549 (wild-type EGFR) and NCI-H1975 (type EGFR of H1975, L858R, and T790M). Using an IC50 of 3.7 μM, the MTT experiment revealed that homoharringtonine was mildly hazardous to A549 cells. With an IC50 of 0.7 μM, homoharringtonine more highly sensitively affected H1975 cells. Using the MTT assay, homoharringtonine exhibited dose- and time-dependent inhibition of A549 and H1975 cell growth and proliferation. Homoharringtonine dramatically reduced the clonogenic potential of A549 and H1975 cells at dose and time [1] according to the trypan blue intermittent test.
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| ln Vivo |
Homoharringtonine (10 mg/kg) successfully stopped the growth of tumors as compared to gefitinib or vehicle control (P<0.05). Furthermore, mice treated with homoharringtonine (HHT) did not lose body weight, suggesting that homoharringtonine has no discernible effect. Every mouse was put to sleep, separated, examined, and tumor samples were gathered. Western blot of tumor-expressing cells will be used to ascertain whether homoharringtonine reduces STAT3 phosphorylation. When compared to the vehicle control or gefitinib treatment groups, the homoharringtonine-treated group exhibited a substantial decrease in both STAT3 phosphorylation and MCL1 levels. In parallel, treatment with harringtonine suppressed the phosphorylation amplifiers for ERK1/2 and AKT1/2/3, which is in line with the results above. Tumor tissues were frozen, and sections were diluted at 10 μM for fluorescence histochemistry in order to investigate STAT3 phosphorylation in deeper detail in xenograft tumor samples that were treated differently. therapy with homoharringtonine suppressed STAT3 phosphorylation more than either gefitinib therapy or tumor immune control [1].
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| References |
[1]. Cao W, et al. Homoharringtonine induces apoptosis and inhibits STAT3 via IL-6/JAK1/STAT3 signal pathway in Gefitinib-resistant lung cancer cells. Sci Rep. 2015 Jul 13;5:8477
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| Molecular Formula |
C29H39NO9
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|---|---|
| Molecular Weight |
545.6213
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| CAS # |
26833-87-4
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| SMILES |
COC1=C[C@@]23[C@H](c4cc(OCO5)c5cc4CCN2CCC3)[C@@H]1OC([C@](O)(CCCC(C)(C)O)CC(OC)=O)=O
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| Chemical Name |
(S)-1-((11bS,12S,14aR)-13-methoxy-2,3,5,6,11b,12-hexahydro-1H-[1,3]dioxolo[4',5'
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| Synonyms |
Omacetaxine mepesuccinate Synribo CGX-635
Myelostat CGX635Ceflatonin homoharringtonine, 3H-labeled,
(3(R))-isomer
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 50 mg/mL (~91.64 mM)
H2O : ~1.4 mg/mL (~2.57 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.58 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.58 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1.67 mg/mL (3.06 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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