Ellipticine hydrochloride (Synonyms: NSC 71795 hydrochloride)

Name: Ellipticine hydrochloride
Brand: MedChemExpress
SKU: HY-15753A
Rating: 4.5 (3 reviews)

Cat. No.: HY-15753A Purity: 99.34%: FAQs
Data Sheet SDS COA Handling Instructions

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Ellipticine (NSC 71795) hydrochloride is a potent antineoplastic agent; inhibits DNA topoisomerase II activities.

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

Ellipticine hydrochloride Chemical Structure

CAS No. : 5081-48-1

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10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
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10 mg	USD 75	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 260	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 380	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Ellipticine hydrochloride:

Ellipticine In-stock

3 Publications Citing Use of MCE Ellipticine hydrochloride

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Topoisomerase Topo I Topo II

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Ellipticine (NSC 71795) hydrochloride is a potent antineoplastic agent; inhibits DNA topoisomerase II activities.

IC₅₀ & Target^[1]

Topoisomerase II

In Vitro

Ellipticine (NSC 71795) is a potent antineoplastic agent exhibiting the multimodal mechanism of its action. The mechanisms of Ellipticine (NSC 71795) antitumor, mutagenic and cytotoxic activities are suggested to be intercalation into DNA and inhibition of DNA topoisomerase II activity. Another mode of Ellipticine (NSC 71795) action is the formation of covalent DNA adducts mediated by its oxidation with cytochromes P450 (CYP) and peroxidases^[1]. Ellipticine (NSC 71795) can also act as an inhibitor or inducer of biotransformation enzymes, thereby modulating its own metabolism leading to its genotoxic and pharmacological effects. Treatment of cells with Ellipticine (NSC 71795) results in inhibition of cell growth and proliferation. This effect is associated with formation of two covalent Ellipticine (NSC 71795)-derived DNA adducts^[2].

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

In Vivo

Ellipticine (NSC 71795) treatment results in ellipticine-derived DNA adduct generation in several healthy organs (liver, kidney, lung, spleen, breast, heart and brain) and in DNA of mammary adenocarcinoma. The levels of Ellipticine (NSC 71795)-derived DNA adducts generated in these adenocarcinomas are almost 2-fold higher than in normal healthy mammary tissue. The induced expression of cytochrome b₅ protein in liver of rats treated with Ellipticine (NSC 71795) suggests that cytochrome b₅ may modulate the CYP-mediated bioactivation and detoxification of Ellipticine (NSC 71795)^[3].

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

Molecular Weight

282.77

Formula

C₁₇H₁₅ClN₂

CAS No.

5081-48-1

Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1=C(C=NC=C2)C2=C(C)C(N3)=C1C4=C3C=CC=C4.Cl

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 5.8 mg/mL (20.51 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.5364 mL	17.6822 mL	35.3644 mL
5 mM	0.7073 mL	3.5364 mL	7.0729 mL
10 mM	0.3536 mL	1.7682 mL	3.5364 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
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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: ≥ 0.84 mg/mL (2.97 mM); Clear solution

This protocol yields a clear solution of ≥ 0.84 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.4 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: ≥ 0.84 mg/mL (2.97 mM); Clear solution

This protocol yields a clear solution of ≥ 0.84 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.4 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: ≥ 0.84 mg/mL (2.97 mM); Clear solution

This protocol yields a clear solution of ≥ 0.84 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 (8.4 mg/mL) to 900 μL Corn oil, and mix evenly.

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 99.34%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (254 KB) LCMS (106 KB)

Handling Instructions (2659 KB)

References

[1]. Stiborova M, et al. Molecular mechanisms of antineoplastic action of an anticancer drug ellipticine. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2006 Jul;150(1):13-23. [Content Brief]

[2]. Stiborova M, et al. Ellipticine cytotoxicity to cancer cell lines - a comparative study. Interdiscip Toxicol. 2011 Jun;4(2):98-105. [Content Brief]

[3]. Stiborova M, et al. The anticancer drug ellipticine activated with cytochrome P450 mediates DNA damage determining its pharmacological efficiencies: studies with rats, Hepatic Cytochrome P450 Reductase Null (HRN?) mice and pure enzymes. Int J Mol Sci. 2014 Dec 25;16(1):284-306. [Content Brief]

Cell Assay
^[2]

The cytotoxicity of Ellipticine (NSC 71795) is determined by MTT test. Ellipticine (NSC 71795) is dissolved in DMSO (1 mM) and diluted in culture medium to final concentrations of 0, 0.1, 1, 5 or 10 μM. Cells in exponential growth are seeded at 1×10⁴ per well in a 96-well microplate. After incubation the MTT solution is added, the microplates are incubated for 4 hours and cells lysed in 50% N,N-dimethylformamide containing 20% of sodium dodecyl sulfate (SDS), pH 4.5. The absorbance at 570 nm is measured. The mean absorbance of medium controls is subtracted as a background. The viability of control cells is taken as 100% and the values of treated cells are calculated as a percentage of control. The IC₅₀ values are calculated using linear regression of the dose-log response curves^[2].

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

References

[1]. Stiborova M, et al. Molecular mechanisms of antineoplastic action of an anticancer drug ellipticine. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2006 Jul;150(1):13-23. [Content Brief]

[2]. Stiborova M, et al. Ellipticine cytotoxicity to cancer cell lines - a comparative study. Interdiscip Toxicol. 2011 Jun;4(2):98-105. [Content Brief]

[3]. Stiborova M, et al. The anticancer drug ellipticine activated with cytochrome P450 mediates DNA damage determining its pharmacological efficiencies: studies with rats, Hepatic Cytochrome P450 Reductase Null (HRN?) mice and pure enzymes. Int J Mol Sci. 2014 Dec 25;16(1):284-306. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.5364 mL	17.6822 mL	35.3644 mL	88.4111 mL
	5 mM	0.7073 mL	3.5364 mL	7.0729 mL	17.6822 mL
	10 mM	0.3536 mL	1.7682 mL	3.5364 mL	8.8411 mL
	15 mM	0.2358 mL	1.1788 mL	2.3576 mL	5.8941 mL
	20 mM	0.1768 mL	0.8841 mL	1.7682 mL	4.4206 mL

Ellipticine hydrochloride 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:

Ellipticine5081-48-1NSC 71795NSC71795NSC-71795TopoisomeraseInhibitorinhibitorinhibit

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Ellipticine hydrochloride (Synonyms: NSC 71795 hydrochloride)

Customer Review

Other Forms of Ellipticine hydrochloride:

Ellipticine hydrochloride Related Antibodies

3 Publications Citing Use of MCE Ellipticine hydrochloride

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Topoisomerase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Ellipticine hydrochloride Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Ellipticine hydrochloride Related Classifications

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