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| Targets |
QN523 acts as an inhibitor of specific enzymes involved in cancer cell signaling pathways. By blocking key molecular targets, the compound aims to prevent tumor growth and spread. The compound induces apoptosis and autophagy in cancer cells. The specific molecular targets of QN523 are not fully detailed in the available literature, but the compound is described as having agent-like properties and potent cytotoxic effects.
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| ln Vitro |
QN523 (72 hours) exhibits cytotoxicity against 12 cell lines, with IC50 values ranging from 0.1 to 5.7 μM[1]. QN523 (0.1 and 0.5 μM; 24 and 48 h; MIA PaCa-2 cells) inhibits the cell cycle at the S phase and postpones the G2-M phase entry of pancreatic cancer cells. QN523 causes MIA PaCa-2 Cells to undergo autophagy and apoptosis[1].
QN523 demonstrates potent in vitro cytotoxicity in a panel of 12 cancer cell lines. The compound induces apoptosis and autophagy. The compound has agent-like properties, suggesting drug-like characteristics. Further detailed in vitro data, including IC50 values against specific cell lines, are available in the primary literature. |
| ln Vivo |
QN523 (10 and 20 mg/kg; ip; daily, for 44 d) prevents the formation of tumors in mice bearing xenografts of pancreatic cancer[1].
QN523 shows significant in vivo efficacy in pancreatic cancer xenograft models. QN523 (10 and 20 mg/kg daily, for 44 days) prevents the formation and growth of tumors. The compound's in vivo efficacy supports its potential as an anticancer agent. |
| Enzyme Assay |
Enzyme inhibition assays for QN523 would involve incubation of the compound with target enzymes and measurement of inhibitory activity. However, specific assay details are not extensively reported in the available literature.
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| Cell Assay |
Cell Cycle Analysis[1]
Cell Types: MIA PaCa-2 cells Tested Concentrations: 0.1 and 0.5 μM Incubation Duration: 24 and 48 hrs (hours) Experimental Results: Delayed for pancreatic cancer cells to enter the G2-M phase because of accumulation of cells in the S phase. Apoptosis Analysis[1] Cell Types: MIA PaCa-2 cells Tested Concentrations: 0.1 and 0.5 μM Incubation Duration: 24 and 48 hrs (hours) Experimental Results: Increased the number of apoptotic cells in time- and dose-dependent manner. Cell-based assays for QN523 are conducted using various cancer cell lines. Cells are treated with the compound at various concentrations, and the following endpoints are assessed: cell viability (by MTT or CellTiter-Glo), apoptosis (by annexin V staining or caspase activation), and autophagy markers. The compound shows potent cytotoxicity in 12 cancer cell lines. |
| Animal Protocol |
Animal/Disease Models: NOD/SCID (severe combined immunodeficient) mouse of pancreatic cancer xenografts (6 weeks of age)
Doses: 10 and 20 mg/kg Route of Administration: intraperitoneal (ip)administration; 1-9 days (10 mg/kg), 10-44 days (20 mg/kg) Experimental Results: Delayed growth of the tumors, and no systemic toxicity. In vivo studies for QN523 are performed in mouse xenograft models, particularly pancreatic cancer xenografts. The compound is administered at 10 and 20 mg/kg daily for 44 days. Pharmacodynamic endpoints include tumor growth inhibition and assessment of apoptosis and autophagy markers in tumor tissues. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of QN523 are not extensively reported in the available literature. The compound has a molecular weight of 250.25-250.26. Storage recommendations include standard conditions for research compounds. The compound is soluble in DMSO and other organic solvents.
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| Toxicity/Toxicokinetics |
As a research compound, QN523 is not intended for human or veterinary use. Standard laboratory safety precautions should be followed when handling the compound, including the use of appropriate personal protective equipment and proper ventilation.
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| References | |
| Additional Infomation |
QN523 is a novel small molecule scaffold with potent in vitro cytotoxicity in 12 cancer cell lines that induces apoptosis and autophagy. The compound has shown significant in vivo efficacy in pancreatic cancer xenograft models. It is being investigated for the treatment of cancers resistant to conventional therapies. The compound is not approved for clinical use and is supplied for research purposes only.
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| Molecular Formula |
C14H10N4O
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| Molecular Weight |
250.26
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| Exact Mass |
250.085
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| CAS # |
878581-60-3
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| PubChem CID |
9463163
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| Appearance |
Light brown to brown solid powder
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| LogP |
1.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
19
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| Complexity |
323
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(C(NC2=C3C(=CC=C2)C=CC=N3)=O)=NC=CN=C1
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| InChi Key |
CYTYVKQBOOTXRP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H10N4O/c19-14(12-9-15-7-8-16-12)18-11-5-1-3-10-4-2-6-17-13(10)11/h1-9H,(H,18,19)
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| Chemical Name |
N-quinolin-8-ylpyrazine-2-carboxamide
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ≥ 16.67 mg/mL (66.61 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9958 mL | 19.9792 mL | 39.9584 mL | |
| 5 mM | 0.7992 mL | 3.9958 mL | 7.9917 mL | |
| 10 mM | 0.3996 mL | 1.9979 mL | 3.9958 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.
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