NQO1-responsive prodrug
NQO1-responsive prodrug is a prodrug of Gemcitabine (dFdC) (HY-17026) with anti-cancer effect. NQO1-responsive prodrug remains stable in plasma and liver/intestinal S9 fractions, releasing dFdC in an NQO1-dependent manner. NQO1-responsive prodrug induces S-phase arrest and apoptosis. NQO1-responsive prodrug inhibits tumor growth in an A549 xenograft mouse model. NQO1-responsive prodrug can be used for breast and non-small cell lung cancer (NSCLC) research.
For research use only. We do not sell to patients.
- Formula: C32H36F2N4O9
- Molecular Weight:658.65
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
NQO1-responsive prodrug (compound 2) (72 h) exhibits antiproliferative activity against both A549 (IC50 = 0.21 μM) and MCF-7 cells (IC50 = 0.49 μM), and demonstrates selectivity towards A549 cells over L02 cells with a selectivity ratio (SR) value of 5.52[1].
NQO1-responsive prodrug (0.08-0.8 μM, 24-36 h) inhibits A549 cell proliferation and migration in a dose-dependent manner, showing excellent antitumor potency in vitro and being more potent than dFdC[1].
NQO1-responsive prodrug (100-400 nM, 24 h) induces S phase cell cycle arrest and apoptosis in A549 cells in a dose-dependent manner[1].
NQO1-responsive prodrug (300 μM, 0-480 min) releases dFdC in an NQO1-dependent manner[1].
NQO1-responsive prodrug exhibits good stability in rat plasma and liver/intestinal S9 fractions[1].
NQO1-responsive prodrug (2 μM, 24 h) is metabolized within A549 cells to produce less of the inactive metabolite dFdU compared to dFdC, and it overcomes the resistance to dFdC due to reduced cellular uptake and increased deamination[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:0.08 and 0.8 μM
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Incubation Time:36 h
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Result:Resulted in a substantial reduction in colony count at the concentration of 0.08 μM.
Showed a complete suppression of colony formation in A549 cells at 0.8 μM.
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Cell Line:A549 cells
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Concentration:0.2 and 0.8 μM
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Incubation Time:24 h
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Result:Showed a dose-dependent inhibition of A549 cell migration.
Demonstrated stronger inhibitory effects compared to dFdC at the same concentration (0.8 μM).
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Cell Line:A549 cells
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Concentration:100, 200, and 400 nM
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Incubation Time:24 h
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Result:Induced apoptosis in tumor cells in a concentration-dependent manner.
Induced apoptosis at a concentration of 100 nM with a rate of 10.6%.
Demonstrated a significantly higher capacity to induce apoptosis than dFdC across the tested concentration range.
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Cell Line:A549 cells
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Concentration:100, 200, and 400 nM
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Incubation Time:24 h
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Result:Dose-dependently induced cell cycle arrest in S phase.
Induced significant S-phase arrest at a much lower concentration (100 nM) than dFdC (400 nM).
| Species | Dose | Route | Note | Tmax | T1/2 | AUC0-t | Vss | MRT | Cmax |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 200 μmol/Kg | i.p. | BALB/c mice,AUC0-12 | 0.50 h | 2.14 h | 2231 ng·h/mL | 192.19 L/kg | 1.97 h | 1182.8 ng/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (3-5 weeks old) subcutaneously injected with A549 cells[1]
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Dosage:0.1 and 0.2 mmol/kg
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Administration:i.p., twice a week for 21 days
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Result:Effectively inhibited tumor growth at a dose of 0.1 mmol/kg, resulting in a TGI value of 55.0% and a treatment/control ratio (T/C) value of 49.9%.
Its antitumor activity was significantly enhanced when the dosage was increased from 0.1 mmol/kg to 0.2 mmol/kg, yielding a TGI of 65.8% and a T/C ratio of 39.1%.
Showed no significant weight loss.
Chemical Information
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Molecular Weight 658.65
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Formula C32H36F2N4O9
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SMILES
O[C@H]1C(F)(F)[C@@H](O[C@@H]1CO)N2C=CC(NC(OCC3=CC=C(N(C)C(CC(C)(C)C4=C(C)C(C(C)=C(C)C4=O)=O)=O)C=C3)=O)=NC2=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NQO1-responsive prodrug Related Classifications
HY-178451 Related Classifications
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