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Art. -Nr.: HY-120825

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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. Nr.: 1527467-32-8
Formel: C₁₆H₁₁N₃O₃
Molecular Weight:293.28

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

QD 232 Chemical Structure

CAS. Nr.: 1527467-32-8

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
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Biologische Aktivität

Beschreibung

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Cellular Effect

Cell Line	Type	Value	Description	References
BXPC-3	IC₅₀	5.2 μM Compound: QD 232	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	[PMID: 29328656]
MIA PaCa-2	IC₅₀	2.3 μM Compound: QD 232	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	[PMID: 29328656]
MIA PaCa-2	IC₅₀	3.6 μM Compound: QD 232	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	[PMID: 29328656]
PANC-1	IC₅₀	0.9 μM Compound: QD 232	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	[PMID: 29328656]

In Vitro

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.

Cell Proliferation Assay^[1]

Cell Line:

MIA PaCa-2, Panc-1, BxPC-3 pancreatic ductal adenocarcinoma (PDAC) cell lines
Concentration:

30 nM - 10 μM
Incubation Time:

72 h
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.

Cell Proliferation Assay^[1]

Cell Line:

gemcitabine-resistant MIA PaCa-2-GR PDAC cell line and HPDE normal pancreatic cell line
Concentration:

30 nM - 10 μM
Incubation Time:

72 h
Result:

Inhibited cell proliferation with an IC₅₀ of 3.6 μM in MIA PaCa-2-GR cells and 4.5 μM in HPDE cells.

Cell Proliferation Assay^[1]

Cell Line:

MIA PaCa-2 PDAC cell line
Concentration:

30 nM - 10 μM; 5 mM NAC (pretreatment)
Incubation Time:

72 h
Result:

Attenuated the proliferation inhibitory effect of QD 232 when cells were pretreated with 5 mM NAC, though protection was not complete.

In Vivo

QD 232 (20 mg/kg; five days on/two days off cycles; 31 days) achieves 65% tumor growth suppression in a MIA PaCa-2 pancreatic ductal adenocarcinoma xenograft model in 6-week-old NOD/SCID mice^[1].

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

Animal Model:

NOD/SCID mice with Pancreatic ductal adenocarcinoma (6-week-old)^[1]
Dosage:

20 mg/kg
Administration:

5 days on/two days off cycles; 31 days
Result:

Suppressed tumor growth by 65% over the 31-day study period.

Chemical Information

CAS. Nr. 1527467-32-8
Molecular Weight 293.28
Formel C₁₆H₁₁N₃O₃
SMILES

O=C1C=C(NC2=CC=CC(=C2)C(=O)C)C(=O)C=3C=NC=NC13
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Kuang Y, et al. Design and Synthesis of Novel Reactive Oxygen Species Inducers for the Treatment of Pancreatic Ductal Adenocarcinoma. J Med Chem. 2018;61(4):1576-1594. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

MOQ

Minimum order quantity

100 mg

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QD 232

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QD 232 Related Classifications

HY-120825 Related Classifications