Voreloxin Hydrochloride
Based on 3 publication(s) in Google Scholar
Voreloxin Hydrochloride is a first-in-class topoisomerase II inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis.
For research use only. We do not sell to patients.
- Purity: 99.58%
- CAS No.: 175519-16-1
- Formula: C18H20ClN5O4S
- Molecular Weight:437.90
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Voreloxin Hydrochloride
MoreAll Topoisomerase Isoforms
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Biological Activity
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Topoisomerase II |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| P388 | IC50 |
0.0075 μg/mL
Compound: 27l(S,S)
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Cytotoxic activity against murine P388 leukemia cells
Cytotoxic activity against murine P388 leukemia cells
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[PMID: 15056007] |
Voreloxin Hydrochloride is a first-in-class topoisomerase II poison and inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis. Voreloxin (0.1-20 µM) inhibits topoisomerase II activity and induces site-selective DNA DSB in CCRF-CEM cells. Voreloxin (0.11, 0.33, 1, 3 µM) induces G2 arrest partially through topoisomerase II in A549 lung cancer cell line. Voreloxin cytotoxic activity requires DNA intercalation. However, Voreloxin (1-9 µM) does not generate significant levels of ROS[1]. Voreloxin has potent cytotoxic activity in AML cell lines MV4-11 and HL-60, with IC50s of 95 ± 8 nM and 884 ± 114 nM, respectively. Voreloxin in combination with cytarabine shows additive or synergistic activity in acute leukemia cell lines[2]. Voreloxin is active on the primary acute myeloid leukemia (AML) with a mean LD50 of 2.3 μM. The LD50 for voreloxin in myeloid cell lines NB4 and HL-60 is 0.59 μM ± 0.25 μM. Voreloxin causes accumulation of cells in the S and G2 phases of the cell cycle and acts on topoisomerase II[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 175519-16-1
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Appearance Solid
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Molecular Weight 437.90
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Formula C18H20ClN5O4S
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Color White to gray
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SMILES
[H]Cl.O=C(C1=CN(C2=NC=CS2)C3=C(C=CC(N4C[C@H](OC)[C@@H](NC)C4)=N3)C1=O)O
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Synonyms
SNS-595 Hydrochloride; Vosaroxin Hydrochloride; AG 7352 Hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Drug Des Devel Ther
Advances in the drug therapies of acute myeloid leukemia (except acute wpromyelocytic leukemia). [Abstract]2018 Apr 30:12:1009-1017. PMID: 29750014 -
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Oncotarget
A novel, dual pan-PIM/FLT3 inhibitor SEL24 exhibits broad therapeutic potential in acute myeloid leukemia. [Abstract]2018 Mar 30;9(24):16917-16931. PMID: 29682194
Solvent & Solubility
DMSO : 2 mg/mL (4.57 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 2 mg/mL (4.57 mM; ultrasonic and warming and heat to 60°C)
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.
* 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.
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.
* 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: PBS
Solubility: 2 mg/mL (4.57 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Protocol
In vitro toxicity assays are performed on primary AML mononuclear cells over a 48 h period using a MTS cell proliferation assay. Lethal doses (LD50) are calculated. Cells are treated with voreloxin (31.25 nM to 4 μM) and Ara-C (62.5 nM to 8 μM) by serial dilution and incubated for 48 h in a final volume of 90 μL. Following the incubation, 20 μL of MTS reagent are added and the reaction is incubated for a further 4 h. The absorbance of the reaction after this time is read by spectrophotometry at 490 nm and the percentage of viable cells calculated relative to untreated control cells in the same assay. IC50 values are calculated using Calcusyn software[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animals are weighed, randomized by body weight, and assigned to the study groups before initiation of treatment. Voreloxin is administered intravenously (IV) at 10 or 20 mg/kg once on day zero and once on day four (q4d ×2). Cytarabine is administered subcutaneously (SC) at 20 or 60 mg/kg every 8 h on day zero and day four (tid q4d ×2). Tissues and blood are sampled on days 6, 8, and 12 from at least three and not greater than ten animals per treatment group. Femurs are placed in Streck Tissue Fixative solution, or in 10% formalin solution for 24-48 h followed by a 70% dehydrant (ethanol, isopropanol, methanol). Femurs are decalcified, paraffin embedded, and sectioned at Biopathology Labs. The four micron sections are stained with hematoxylin-eosin (H&E). H&E stained femurs are examined and percent cellularity of the bone marrow is determined. Digital photographs of representative femur sections are taken on a Leica DM2000 microscope using Image-Pro Plus v6.1 software[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Hotinski AK, et al. Vosaroxin is a novel topoisomerase-II inhibitor with efficacy in relapsed and refractory acute myeloid leukaemia. Expert Opin Pharmacother. 2015 Jun;16(9):1395-402. [Content Brief]
[2]. Scatena CD, et al. Voreloxin, a first-in-class anticancer quinolone derivative, acts synergistically with cytarabine in vitro and induces bone marrow aplasia in vivo. Cancer Chemother Pharmacol. 2010 Oct;66(5):881-8. [Content Brief]
[3]. Walsby EJ, et al. The topoisomerase II inhibitor voreloxin causes cell cycle arrest and apoptosis in myeloid leukemia cells and acts in synergy with cytarabine. Haematologica. 2011 Mar;96(3):393-9. [Content Brief]
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.2836 mL | 11.4181 mL | 22.8363 mL | 57.0907 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.