Homoharringtonine (Synonyms: Omacetaxine mepesuccinate; HHT)

Name: Homoharringtonine
Brand: MedChemExpress
SKU: HY-14944
Rating: 5.0 (21 reviews)

Cat. No.: HY-14944 Purity: 99.75%: FAQs
Data Sheet SDS COA Handling Instructions

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

For research use only. We do not sell to patients.

Homoharringtonine Chemical Structure

CAS No. : 26833-87-4

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 84	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 84	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 112	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 383	In-stock	Estimated Time of Arrival: December 31
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200 mg		Get quote

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Based on 21 publication(s) in Google Scholar

20 Publications Citing Use of MCE Homoharringtonine

: Homoharringtonine purchased from MedChemExpress. 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.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

IC₅₀ & Target^[1]

STAT3

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 IC₅₀ of 3.7 μM and H1975 cells are more sensitive to Homoharringtonine with an IC₅₀ of 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].

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

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].

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

Clinical Trial

Molecular Weight

545.62

Formula

C₂₉H₃₉NO₉

CAS No.

26833-87-4

Appearance

Solid

Color

Off-white to yellow

SMILES

[H][C@@]12[C@](CCC3)(C=C(OC)[C@]2(OC([C@](CCCC(O)(C)C)(O)CC(OC)=O)=O)[H])N3CCC4=CC5=C(OCO5)C=C14

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (91.64 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 1.67 mg/mL (3.06 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.96%

Select Batch:

Data Sheet (289 KB) SDS (0 KB)

COA (262 KB) HNMR (300 KB) LCMS (114 KB)

Handling Instructions (2659 KB)

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 [Content Brief]

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.
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 [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Homoharringtonine Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
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.

Keywords:

Homoharringtonine26833-87-4Omacetaxine mepesuccinate HHTSTATInhibitorinhibitorinhibit

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Homoharringtonine (Synonyms: Omacetaxine mepesuccinate; HHT)

Customer Review

Homoharringtonine Related Antibodies

20 Publications Citing Use of MCE Homoharringtonine

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All STAT Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Homoharringtonine Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Homoharringtonine Related Classifications

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