2. Apoptosis
  3. Apoptosis
  4. 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.

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NQO1-responsive prodrug

NQO1-responsive prodrug Chemical Structure

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NQO1-responsive prodrug Related Antibodies

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Description

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[1].

In Vitro

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.

NQO1-responsive prodrug Related Antibodies

Cell Proliferation Assay[1]

Cell Line: A549 cells
Concentration: 0.08 and 0.8 μM
Incubation Time: 36 h
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.

Cell Migration Assay [1]

Cell Line: A549 cells
Concentration: 0.2 and 0.8 μM
Incubation Time: 24 h
Result: Showed a dose-dependent inhibition of A549 cell migration.
Demonstrated stronger inhibitory effects compared to dFdC at the same concentration (0.8 μM).

Apoptosis Analysis[1]

Cell Line: A549 cells
Concentration: 100, 200, and 400 nM
Incubation Time: 24 h
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.

Cell Cycle Analysis[1]

Cell Line: A549 cells
Concentration: 100, 200, and 400 nM
Incubation Time: 24 h
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).
In Vivo

NQO1-responsive prodrug (0.1 and 0.2 mmol/kg, i.p., twice a week for 21 days) significantly reduces tumor volume without affecting body weight in A549 xenograft mouse model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice (3-5 weeks old) subcutaneously injected with A549 cells[1]
Dosage: 0.1 and 0.2 mmol/kg
Administration: i.p., twice a week for 21 days
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.
Molecular Weight

658.65

Formula

C32H36F2N4O9
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
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NQO1-responsive prodrug Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NQO1-responsive prodrugApoptosisGemcitabineprodrugdFdCNQO1A549MCF-7breastNSCLCInhibitorinhibitorinhibit

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