| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Abl (IC50 = 0.6 nM); Src (IC50 = 0.8 nM); c-Kit (D816V) (IC50 = 37 nM); c-Kit (wt) (IC50 = 79 nM)
Quarfloxin's primary target is the RNA polymerase I (RNA pol I) transcription machinery. It binds to G-quadruplex DNA structures in the ribosomal DNA (rDNA) template, disrupting the interaction between rDNA G-quadruplexes and nucleolin. This inhibits RNA pol I-mediated transcription and rRNA biogenesis. |
|---|---|
| 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]. In vitro, Quarfloxin inhibits RNA polymerase I activity with IC50 values in the nanomolar range in neuroblastoma cells. It binds to G-quadruplex DNA and disrupts the interaction with nucleolin. |
| ln Vivo |
In vivo, Quarfloxin has been investigated in clinical trials as an anticancer agent. Its mechanism of action involves disrupting ribosomal RNA (rRNA) biogenesis.
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| Enzyme Assay |
The in vitro activity of Quarfloxin is assessed using cell-free assays measuring RNA polymerase I activity. The enzyme is incubated with its DNA template and substrates in the presence of varying concentrations of Quarfloxin. The incorporation of labeled nucleotides into RNA is measured.
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| Cell Assay |
For cellular assays, cancer cell lines, such as neuroblastoma cells, are used. Cells are treated with various concentrations of Quarfloxin, and the inhibition of rRNA synthesis, cell proliferation, and induction of apoptosis are assessed.
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| Animal Protocol |
In vivo, Quarfloxin is typically administered to patients in clinical trials. Its efficacy is assessed by measuring tumor response and other clinical outcomes.
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| ADME/Pharmacokinetics |
Quarfloxin has a molecular weight of 604.67 g/mol and a molecular formula of C35H33FN6O3. It is a fluoroquinolone analogue.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Quarfloxin is not detailed in the provided search results. As an investigational compound, its safety profile would be established through clinical trials.
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| References | |
| Additional Infomation |
Itarnafloxin is a phenoxazine drug. Quarfluoxetine is a fluoroquinolone derivative with antitumor activity. Quarfluoxetine disrupts the interaction between nucleolar proteins and the G-quadruplex DNA structure in the ribosomal DNA (rDNA) template. This interaction is crucial for rRNA biosynthesis and is overexpressed in cancer cells; disruption of the G-quadruplex DNA-protein interaction in abnormal rRNA biosynthesis may lead to ribosome inhibition and tumor cell apoptosis.
Drug Indications It has been studied for the treatment of lymphocytic leukemia. Quarfloxin is an investigational anticancer agent that has been studied in clinical trials. Its mechanism of action involves targeting G-quadruplex DNA structures and inhibiting rRNA biogenesis. This novel mechanism differentiates it from conventional cytotoxic chemotherapeutics. |
| Molecular Formula |
C35H33FN6O3
|
|---|---|
| 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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