Voreloxin (SNS-595) hydrochloride

Catalog No.S7518 Batch:S751801

Technical Data

Formula	C₁₈H₂₀ClN₅O₄S
Molecular Weight	437.9	CAS No.	175519-16-1
Solubility (25°C)*	In vitro	DMSO	20 mg/mL (45.67 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Voreloxin hydrochloride (SNS-595, Vosaroxin) is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2.

Targets

Topo II ^[1]

In vitro

Voreloxin exhibits potent inhibitory effect in topoisomerase II relaxation with IC50 of 3.2 μg /mL without effect on topoisomerase II cleavage. Voreloxin has a cytotoxic activity against human tumor cell lines more potent than that of etoposide. ^[1] Voreloxin has broad anti-proliferative activity in 15 cell lines, including 4 drug-resistant lines, with IC50 ranging from 0.04 to 1.155 μM. ^[2]

In vivo

Voreloxin (50 mg/kg i.p.) shows potent in vivo antitumor activity mice implanted with P388 leukemia cells. ^[1] Voreloxin (25 mg/kg i.v.) demonstrates strong tumor growth inhibition in 10 of 11 solid tumor (breast, ovarian, colon, lung, gastric, and melanoma) xenograft models, 2 hematologic tumor xenograft models, 3 multidrug resistant tumor models and 3 murine syngeneic tumor models (Colon 26, Lewis Lung carcinoma, M5076 Ovarian Sarcoma). ^[2]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines P388 leukemia cells Concentrations ~10 μg/mL Incubation Time 72 hours Method Cells are put into wells of a 96-well microtiter plate in the amount of 0.1 mL/well, preincubated for 24 h except for P388 cells, and incubated with various concentrations of a test compound in the 5% CO₂ incubator at 37 ° for 72 h. After the culturing, 0.02 mL of a MTT solution (5 mg/mL) is put in each well, and the cells are cultured for a further 4 h. The medium is removed by suction, and 0.2 mL of DMSO is put in each well to dissolve the formed formazan. The absorbance is measured by Multiskan Bichromatic. The IC50 is defined as the drug concentration needed to produce a 50% reduction of absorbance relative to the control.
Animal Study:^{^[1]}	Animal Models Mice implanted with P388 leukemia cells. Dosages ~50 mg/kg Administration i.p.

Cell Assay:^{^[1]}

Cell lines
P388 leukemia cells
Concentrations
~10 μg/mL
Incubation Time
72 hours
Method
Cells are put into wells of a 96-well microtiter plate in the amount of 0.1 mL/well, preincubated for 24 h except for P388 cells, and incubated with various concentrations of a test compound in the 5% CO₂ incubator at 37 ° for 72 h. After the culturing, 0.02 mL of a MTT solution (5 mg/mL) is put in each well, and the cells are cultured for a further 4 h. The medium is removed by suction, and 0.2 mL of DMSO is put in each well to dissolve the formed formazan. The absorbance is measured by Multiskan Bichromatic. The IC50 is defined as the drug concentration needed to produce a 50% reduction of absorbance relative to the control.

Animal Study:^{^[1]}

Animal Models
Mice implanted with P388 leukemia cells.
Dosages
~50 mg/kg
Administration
i.p.

References

Selleck's Voreloxin (SNS-595) hydrochloride has been cited by 7 publications

Topoisomerase II as a Novel Antiviral Target against Panarenaviral Diseases [ Viruses, 2022, 15(1)105]	PubMed: 36680145
KEAP1 Mutations Drive Tumorigenesis by Suppressing SOX9 Ubiquitination and Degradation [ Adv Sci (Weinh), 2020, 7(21):2001018]	PubMed: 33173725
Combination of ERK2 inhibitor VX-11e and voreloxin synergistically enhances anti-proliferative and pro-apoptotic effects in leukemia cells [ Apoptosis, 2019, 24(11-12):849-861]	PubMed: 31482470
Venetoclax Synergistically Enhances the Anti-leukemic Activity of Vosaroxin Against Acute Myeloid Leukemia Cells Ex Vivo. [ Target Oncol, 2019, 14(3):351-364]	PubMed: 31115744
Predicting effective pro-apoptotic anti-leukaemic drug combinations using co-operative dynamic BH3 profiling [ PLoS One, 2018, 13(1):e0190682]	PubMed: 29298347
Early changes in rpS6 phosphorylation and BH3 profiling predict response to chemotherapy in AML cells. [ PLoS One, 2018, 13(5):e0196805]	PubMed: 29723246
TAK-733, a Selective MEK Inhibitor, Enhances Voreloxin-induced Apoptosis in Myeloid Leukemia Cells [ Anticancer Res, 2018, 38(11):6147-6156]	PubMed: 30396931

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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