ChemicalBook CAS DataBase List 175519-16-1

175519-16-1

Name	AG 7352 Hydrochloride
CAS	175519-16-1
Molecular Formula	C18H20ClN5O4S
MDL Number	MFCD00946608
Molecular Weight	437.9
MOL File	175519-16-1.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	Soluble in DMSO
form	Solid
color	White to gray
Optical Rotation	[α]/D +42 to +52°, c =1 in 0.1 M NaOH
Water Solubility	H2O: 1mg/mL, clear (warmed)
InChIKey	JJZCCQHWCOXGCL-QNTKWALQSA-N
SMILES	O=C(C(C(O)=O)=C1)C2=C(N=C(C=C2)N3C[C@@H]([C@H](C3)NC)OC)N1C4=NC=CS4

Safety Data

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Hazard Information

Uses

Voreloxin Hydrochloride is a first-in-class topoisomerase II inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis.

Biological Activity

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

in vivo

Voreloxin (20 mg/kg, i.v.) alone results in 80% reduction in bone marrow cellularity of CD-1 mice by administration one dose every 4 days repeated twice (q4d ×2). voreloxin at 10 mg/kg in combination with cytarabine causes ablation of the marrow, dilation of sinusoids, and infiltration of adipocytes in mice. Voreloxin (20 mg/kg, i.v.) combined with cytarabine causes a reversible decrease in myeloid and lymphoid cells in bone marrow and peripheral blood CD-1 mice. voreloxin (10 mg/kg, q4d ×2) and cytarabine in combination causes reversible neutropenia with a more modest impact on platelets CD-1 mice^[2].

target

Target	Value
Topo II

IC 50

Topoisomerase II

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. DOI:10.1517/14656566.2015.1044437
[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. DOI:10.1007/s00280-009-1234-z
[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. DOI:10.3324/haematol.2010.032680

Spectrum Detail

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