Quarfloxin
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MedKoo CAT#: 202380

CAS#: 865311-47-3

Description: Quarfloxin, also known as Quarfloxacin and CX-3543, is a fluoroquinolone derivative with antineoplastic activity. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template, a critical interaction for rRNA biogenesis that is overexpressed in cancer cells; disruption of this G-quadruplex DNA:protein interaction in aberrant rRNA biogenesis may result in the inhibition of ribosome synthesis and tumor cell apoptosis.


Chemical Structure

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Quarfloxin
CAS# 865311-47-3

Theoretical Analysis

MedKoo Cat#: 202380
Name: Quarfloxin
CAS#: 865311-47-3
Chemical Formula: C35H33FN6O3
Exact Mass: 604.26
Molecular Weight: 604.670
Elemental Analysis: C, 69.52; H, 5.50; F, 3.14; N, 13.90; O, 7.94

Price and Availability

Size Price Availability Quantity
5mg USD 550 2 Weeks
10mg USD 950 2 Weeks
50mg USD 2450 2 Weeks
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Synonym: CX 3543; CX-3543; CX 3543; Quarfloxacin

IUPAC/Chemical Name: 5-fluoro-N-(2-((S)-1-methylpyrrolidin-2-yl)ethyl)-3-oxo-6-((R)-3-(pyrazin-2-yl)pyrrolidin-1-yl)-3H-benzo[b]pyrido[3,2,1-kl]phenoxazine-2-carboxamide.

InChi Key: WOQIDNWTQOYDLF-RPWUZVMVSA-N

InChi Code: InChI=1S/C35H33FN6O3/c1-40-13-4-7-24(40)8-10-39-35(44)26-20-42-29-15-21-5-2-3-6-22(21)16-30(29)45-34-31(42)25(33(26)43)17-27(36)32(34)41-14-9-23(19-41)28-18-37-11-12-38-28/h2-3,5-6,11-12,15-18,20,23-24H,4,7-10,13-14,19H2,1H3,(H,39,44)/t23-,24+/m1/s1

SMILES Code: O=C(C1=CN2C3=C(C(N4C[C@H](C5=NC=CN=C5)CC4)=C(F)C=C3C1=O)OC6=CC7=CC=CC=C7C=C26)NCC[C@H]8N(C)CCC8

Appearance: solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Clinical trial news:  Quarfloxin is a ground-breaking small-molecule targeted cancer therapeutic derived from the validated fluoroquinolone class of drugs. Rationally designed to selectively inhibit ribosomal RNA (rRNA) biogenesis in cancer cells, quarfloxin disrupts the interaction between the Nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template, a critical interaction for rRNA biogenesis and one that is amplified in cancer cells. As a result, quarfloxin selectively induces apoptotic cell death in cancers. Many commercialized cancer therapeutics act indirectly on rRNA Biogenesis through upstream modulators, but quarfloxin is the first agent to directly target this cancer-specific aberrant cell function. According to  news released on June 19, 2011, Cylene Pharmaceuticals announced the initiation of a Phase II clinical trial of quarfloxin (CX-3543) in patients with carcinoid/neuroendocrine tumors (C/NET), which are malignant cancers arising from neural crest cells.   

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 604.67 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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