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Quarfloxin (Quarfloxacin; CX-3543) is a novel and potent fluoroquinolone analogue with anticancer activity. In order to cause rRNA biogenesis, quarfloxin works by interfering with the nucleolin protein's attachment to a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template. This interaction is overexpressed in cancer cells. When this G-quadruplex DNA:protein interaction in aberrant rRNA biogenesis is disrupted, tumor cell apoptosis and ribosome synthesis may be inhibited.
| Targets |
Abl (IC50 = 0.6 nM); Src (IC50 = 0.8 nM); c-Kit (D816V) (IC50 = 37 nM); c-Kit (wt) (IC50 = 79 nM)
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|---|---|
| ln Vitro |
Quarfloxin (CX-3543) effectively prevents neuroblastoma cell growth in vitro. It is discovered that wt-TP53 and MNA (or high c-Myc) cell lines are more susceptible to Quarfloxin. Quarfloxin causes cell death, cell cycle arrest, DNA damage, and p53 signaling in neuroblastoma cell lines[1].
Quarfloxin is suspended in DMSO to a stock of 10 mM as an in vitro solution[1]. |
| References | |
| Additional Infomation |
Itarnafloxin is a phenoxazine.
Quarfloxin 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. Drug Indication Investigated for use/treatment in leukemia (lymphoid). |
| Molecular Formula |
C35H33FN6O3
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|---|---|
| Molecular Weight |
604.67
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| Exact Mass |
604.259
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| Elemental Analysis |
C, 69.52; H, 5.50; F, 3.14; N, 13.90; O, 7.94
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| CAS # |
865311-47-3
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| Related CAS # |
865311-47-3
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| PubChem CID |
11635763
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
845.3±65.0 °C at 760 mmHg
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| Flash Point |
465.0±34.3 °C
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| Vapour Pressure |
0.0±3.1 mmHg at 25°C
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| Index of Refraction |
1.732
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| LogP |
2.97
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
45
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| Complexity |
1150
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O=C1C(C(=O)NCC[C@H]2N(C)CCC2)=CN2C3C=C4C=CC=CC4=CC=3OC3C2=C1C=C(F)C=3N1CCC(C2N=CC=NC=2)C1
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| InChi Key |
WOQIDNWTQOYDLF-CGAIIQECSA-N
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| 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-/m0/s1
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| Chemical Name |
15-fluoro-N-[2-[(2S)-1-methylpyrrolidin-2-yl]ethyl]-18-oxo-14-(3-pyrazin-2-ylpyrrolidin-1-yl)-12-oxa-1-azapentacyclo[11.7.1.02,11.04,9.017,21]henicosa-2,4,6,8,10,13(21),14,16,19-nonaene-19-carboxamide
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| Synonyms |
CX 3543; CX-3543; CX 3543
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 5~100 mg/mL (8.3~197.6 mM)
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|---|---|
| Solubility (In Vivo) |
2% DMSO+30% PEG 300+dd H2O: 5mg/mL (Please use freshly prepared in vivo formulations for optimal results.)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6538 mL | 8.2690 mL | 16.5379 mL | |
| 5 mM | 0.3308 mL | 1.6538 mL | 3.3076 mL | |
| 10 mM | 0.1654 mL | 0.8269 mL | 1.6538 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00780663 | Completed | Drug: Quarfloxin | Neuroendocrine Tumors Carcinoid Tumor |
Cylene Pharmaceuticals | October 2008 | Phase 2 |
| NCT00955786 | Completed | Drug: CX-3543 | Advanced Solid Tumors Lymphoma |
Cylene Pharmaceuticals | July 2005 | Phase 1 |
| NCT00955292 | Completed | Drug: Quarfloxin | Advanced Solid Tumors Lymphoma |
Cylene Pharmaceuticals | July 2007 | Phase 1 |
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