HY-14944-10mg | Homoharringtonine [26833-87-4] Biotrend

Description

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

IC₅₀ & Target^[1]

STAT3

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	0.06 μM Compound: 1; HHT	Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
A204	IC₅₀	0.004 μM Compound: 1; HHT	Antiproliferative activity against human A204 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human A204 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
A549	IC₅₀	0.03 μM Compound: Homoharringtonine	Cytotoxicity against human A549 cells assessed as reduction of cell growth by SRB method Cytotoxicity against human A549 cells assessed as reduction of cell growth by SRB method	[PMID: 18782668]
A549	IC₅₀	18.28 nM Compound: HHT	Inhibition of Nuclear factor erythroid 2-related factor 2 5'-untranslated region guanine-rich DNA sequence in human A549 cells harboring ARE-GFP-Luc assessed as reduction in ARE-luciferase activity after 24 hrs by firefly luciferase reporter gene assay Inhibition of Nuclear factor erythroid 2-related factor 2 5'-untranslated region guanine-rich DNA sequence in human A549 cells harboring ARE-GFP-Luc assessed as reduction in ARE-luciferase activity after 24 hrs by firefly luciferase reporter gene assay	[PMID: 31270017]
A549	IC₅₀	31.6 nM Compound: homoharringtonine	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 31916761]
BaF3	IC₅₀	0.081 μM Compound: 1; HHT	Antiproliferative activity against mouse BaF3 cells expressing Bcr/Abl-T315I mutant assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing Bcr/Abl-T315I mutant assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
Caco-2	CC₅₀	1.72 μM Compound: HOMOHARRINGTONINE	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay	10.21203/rs.3.rs-23951/v1
Caco-2	IC₅₀	4.71 μM Compound: HOMOHARRINGTONINE	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging	10.21203/rs.3.rs-23951/v1
HCT-116	IC₅₀	0.013 μM Compound: 1; HHT	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
HeLa	IC₅₀	0.4 μM Compound: Homoharringtonine	Cytotoxicity against human HeLa cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 33905250]
HeLa	IC₅₀	1.7 μM Compound: HHT	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 68 hrs by MTS assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 68 hrs by MTS assay	[PMID: 35148094]
HepG2	IC₅₀	34.5 nM Compound: homoharringtonine	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 31916761]
HL-60	IC₅₀	0.013 μM Compound: 1; HHT	Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
HL-60	IC₅₀	0.02 μM Compound: homoharringtonine	Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by Alamar Blue assay Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by Alamar Blue assay	10.1039/C0MD00241K
HL-60	IC₅₀	0.022 μM Compound: HHT	Antiproliferative activity against human HL60 cells after 62 hrs by MTS assay Antiproliferative activity against human HL60 cells after 62 hrs by MTS assay	[PMID: 29286665]
HL-60	IC₅₀	21.8 nM Compound: HHT	Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth measured after 68 hrs by MTS assay Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth measured after 68 hrs by MTS assay	[PMID: 35148094]
Huh-7	IC₅₀	0.04 μM Compound: 1; HHT	Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
K562	IC₅₀	0.014 μM Compound: 1; HHT	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
KB	IC₅₀	0.004 μM Compound: Homoharringtonine	Cytotoxicity against human KB cells assessed as reduction of cell growth by SRB method Cytotoxicity against human KB cells assessed as reduction of cell growth by SRB method	[PMID: 18782668]
L02	IC₅₀	0.064 μM Compound: 1; HHT	Cytotoxicity against human HL7702 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Cytotoxicity against human HL7702 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
MDA-MB-453	IC₅₀	0.021 μM Compound: 1; HHT	Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
MOLT-4	IC₅₀	0.007 μM Compound: 1; HHT	Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
MV4-11	IC₅₀	0.005 μM Compound: 1; HHT	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
NCI-H1299	IC₅₀	0.022 μM Compound: 1; HHT	Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
NCI-H1975	IC₅₀	0.022 μM Compound: 1; HHT	Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
NCI-H716	IC₅₀	0.065 μM Compound: 1; HHT	Antiproliferative activity against human NCI-H716 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H716 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
OCI-Ly3	IC₅₀	0.005 μM Compound: 1; HHT	Antiproliferative activity against human OCILY3 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human OCILY3 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
U-937	IC₅₀	0.012 μM Compound: 1; HHT	Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]

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

08[C@@]12[C@](CCC3)(C=C(OC)[C@]2(OC([C@](CCCC(O)(C)C)(O)CC(OC)=O)=O)08)N3CCC4=CC5=C(OCO5)C=C14

Structure Classification

Alkaloids
Pyrrole Alkaloids

Initial Source

Plants
Cephalotaxaceae
Cephalotaxus fortunei Hooker

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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:

SDS (420 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

Cancer
Cancer Targeted Therapy Cancer Immunotherapy Cancer Stem Cells Cancer Drug Resistance

JAK/STAT Signaling Stem Cell/Wnt
STAT

Homoharringtonine [26833-87-4]

Cat# HY-14944-10mg

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Complete Stock Solution Preparation Table

Homoharringtonine Related Classifications

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Homoharringtonine [26833-87-4]

Cat# HY-14944-10mg

Contact local distributor :

Brand : MedChemExpress

Contact local distributor :

Other Forms of Homoharringtonine:

View All STAT Isoform Specific Products:

Homoharringtonine Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Homoharringtonine Related Classifications

Keywords:

You might also be interested by the following products: