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Vosaroxin

Vosaroxin structure

CAS No:
175414-77-4
Formula:
C18H19N5O4S
Chemical Name:
Vosaroxin
Synonyms:
1,8-Naphthyridine-3-carboxylic acid,1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-;1,8-Naphthyridine-3-carboxylic acid,1,4-dihydro-7-[3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-,(3S-trans)-;1,4-Dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid;(+)-AG-7352;AG 7352;SNS 595;SPC 595;Vosaroxin
Categories:
Biochemical Engineering > Inhibitors

Description

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

Vosaroxin is under investigation for the treatment of Leukemia, Myeloid, Acute.|Vosaroxin is a small molecule and a naphthyridine analogue with antineoplastic activity. Vosaroxin intercalates into DNA in a site-specific manner and blocks the re-ligation process carried out by topoisomerase II during DNA replication. As a result, inhibition of DNA replication, RNA and protein synthesis occurs, followed by cell cycle arrest at G2 phase and induced p53-independent apoptosis. This agent shows a favorable toxicity profile in several aspects: it does not generate reactive oxygen species, as do anthracyclines, hence reducing the risk of cardiotoxicity; it is not a P-glycoprotein (P-gp) substrate, and thereby evades the common mechanism for multidrug resistance; and it has limited distribution to normal tissues and a more chemically stable molecular structure.

Vosaroxin Basic Attributes

Molecular Weight：

401.441

Exact Mass：

401.44

UNII：

K6A90IIZ19

NCI Thesaurus Code：

C95148

ATC Code：

L - Antineoplastic and immunomodulating agents

Characteristics

PSA：

136

XLogP3：

-0.51

Density：

1.5±0.1 g/cm3

Boiling Point：

652.0±65.0 °C at 760 mmHg

Flash Point：

348.1±34.3 °C

Refractive Index：

1.703

Drug Information

Drug Indication：

Treatment of acute myeloid leukaemia

MeSH Entry Terms：

1,4-dihydro-7-(3-methoxy-4-methylamino-1-pyrrolidinyl)-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid

Vosaroxin Use and Manufacturing

Use Classification：

Human drugs -> Rare disease (orphan)|Human Drugs -> EU pediatric investigation plans

Computed Properties

Molecular Weight:401.4
XLogP3:-0.3
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:10
Rotatable Bond Count:5
Exact Mass:401.11577528
Monoisotopic Mass:401.11577528
Topological Polar Surface Area:136
Heavy Atom Count:28
Complexity:662
Defined Atom Stereocenter Count:2
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Recommended Suppliers of Vosaroxin

Henan Lihao Chem Plant Limited Contact Supplier

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CAS No.: 175414-77-4

Grade: Industrial Grade

Content: 99%

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