QD 232
QD 232 is a quinazolinedione-based ROS inducer and an apoptosis inducer with cytotoxicity and redox regulatory activity. QD 232 promotes ROS accumulation, activates the NRF2-mediated oxidative stress response and unfolded protein response pathways, and upregulates downstream antioxidant and stress response genes. QD 232 inhibits mtDNA transcription driven by HSP2 and LSP promoters, and impairs mitochondrial oxidative phosphorylation function. QD 232 induces apoptosis of pancreatic ductal adenocarcinoma cells and exerts cytotoxicity against gemcitabine (HY-17026)-resistant pancreatic ductal adenocarcinoma cells. QD 232 delays tumor growth in a mouse pancreatic cancer xenograft model.
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- CAS No.: 1527467-32-8
- Formule: C16H11N3O3
- Masse moléculaire:293.28
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BXPC-3 | IC50 |
5.2 μM
Compound: QD 232
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Cytotoxicity against human BxPC3 cells assessed as decrease in cell proliferation after 72 hrs by MTT assay
Cytotoxicity against human BxPC3 cells assessed as decrease in cell proliferation after 72 hrs by MTT assay
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[PMID: 29328656] |
| MIA PaCa-2 | IC50 |
2.3 μM
Compound: QD 232
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Cytotoxicity against human MIAPaCa2 cells assessed as decrease in cell proliferation after 72 hrs by MTT assay
Cytotoxicity against human MIAPaCa2 cells assessed as decrease in cell proliferation after 72 hrs by MTT assay
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[PMID: 29328656] |
| MIA PaCa-2 | IC50 |
3.6 μM
Compound: QD 232
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Cytotoxicity against gemcitabine-resistant human MIAPaCa2 cells assessed as decrease in cell proliferation after 72 hrs by MTT assay
Cytotoxicity against gemcitabine-resistant human MIAPaCa2 cells assessed as decrease in cell proliferation after 72 hrs by MTT assay
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[PMID: 29328656] |
| PANC-1 | IC50 |
0.9 μM
Compound: QD 232
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Cytotoxicity against human PANC1 cells assessed as decrease in cell proliferation after 72 hrs by MTT assay
Cytotoxicity against human PANC1 cells assessed as decrease in cell proliferation after 72 hrs by MTT assay
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[PMID: 29328656] |
QD 232 (30 nM - 10 μM; 72 h) inhibits proliferation of MIA PaCa-2, Panc-1, and BxPC-3 PDAC cell lines with IC50 values of 2.3 μM, 0.9 μM, and 5.2 μM, respectively[1].
QD 232 (30 nM - 10 μM; 72 h) inhibits proliferation of gemcitabine-resistant MIA PaCa-2-GR cells and normal HPDE pancreatic cells with IC50 values of 3.6 μM and 4.5 μM, respectively[1].
QD 232 (30 nM - 10 μM; 72 h) has its proliferation inhibitory effect in MIA PaCa-2 cells attenuated by pretreatment with 5 mM NAC (HY-B0215)[1].
QD 232 treatment induces time-dependent increases in CHOP and GRP78 protein levels in MIA PaCa-2, Panc-1, and BxPC-3 cells, upregulates HO-1 protein in MIA PaCa-2 and BxPC-3 cells, and does not induce NQO1 protein in MIA PaCa-2 and BxPC-3 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MIA PaCa-2, Panc-1, BxPC-3 pancreatic ductal adenocarcinoma (PDAC) cell lines
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Concentration:30 nM - 10 μM
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Incubation Time:72 h
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Result:Inhibited cell proliferation with IC50 values of 2.3 μM in MIA PaCa-2 cells, 0.9 μM in Panc-1 cells, and 5.2 μM in BxPC-3 cells.
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Cell Line:gemcitabine-resistant MIA PaCa-2-GR PDAC cell line and HPDE normal pancreatic cell line
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Concentration:30 nM - 10 μM
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Incubation Time:72 h
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Result:Inhibited cell proliferation with an IC50 of 3.6 μM in MIA PaCa-2-GR cells and 4.5 μM in HPDE cells.
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Cell Line:MIA PaCa-2 PDAC cell line
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Concentration:30 nM - 10 μM; 5 mM NAC (pretreatment)
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Incubation Time:72 h
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Result:Attenuated the proliferation inhibitory effect of QD 232 when cells were pretreated with 5 mM NAC, though protection was not complete.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID mice with Pancreatic ductal adenocarcinoma (6-week-old)[1]
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Dosage:20 mg/kg
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Administration:5 days on/two days off cycles; 31 days
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Result:Suppressed tumor growth by 65% over the 31-day study period.
Chemical Information
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CAS No. 1527467-32-8
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Masse moléculaire 293.28
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Formule C16H11N3O3
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SMILES
O=C1C=C(NC2=CC=CC(=C2)C(=O)C)C(=O)C=3C=NC=NC13
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
QD 232 Related Classifications
HY-120825 Related Classifications
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