Anticancer agent 309
Anticancer agent 309 (Compound HZ-1) is an anticancer agent and G-quadruplex binder, with Kd values of 2.46 μM and 1.61 μM for c-Myc G4 and KRAS G4, respectively. Anticancer agent 309 promotes the formation of intranuclear G4. Anticancer agent 309 shows higher selectivity for parallel G4 than for non-parallel G4. Anticancer agent 309 inhibits the NRF2 signaling pathway and reduces the expression of XCT and GPX4. Anticancer agent 309 induces Ferroptosis, Apoptosis and immunogenic cell death in cells. Anticancer agent 309 exerts antitumor efficacy against breast cancer. Anticancer agent 309 is applicable for the research of breast cancer.
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- Formule: C31H36N6
- Masse moléculaire:492.66
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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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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Anticancer agent 309 binds potently to purified c-Myc G4 and KRAS G4 structures, with Kd values of 2.46 μM and 1.61 μM, respectively[1].
Anticancer agent 309 (24 h) inhibits the proliferation of various human and mouse tumor cell lines (MDA-MB-231, HCT116, HepG2, A549, MCF-7, 4T1), with IC50 values ranging from 7.77 ± 0.77 μM to 16.71 ± 0.71 μM[1].
Anticancer agent 309 (10 μM; 24 h) promotes the formation of nuclear G4 in human breast cancer MDA-MB-231 cells[1].
Anticancer agent 309 (5-20 μM; 24 h) triggers apoptosis in breast cancer MDA-MB-231 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human breast cancer MDA-MB-231 cells, human colon cancer HCT116 cells, human liver cancer HepG2 cells, human lung cancer A549 cells, human breast cancer MCF-7 cells, mouse breast cancer 4T1 cells, human normal breast MCF-10a cells
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Concentration:Titrated to determine IC50
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Incubation Time:24 h
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Result:Exerted dose-dependent cytotoxicity against all tested tumor cell lines, with IC50 values of 7.77 ± 0.77 μM (MDA-MB-231), 8.33 ± 0.46 μM (HCT116), 9.88 ± 1.18 μM (HepG2), 11.67 ± 0.33 μM (A549), 16.71 ± 0.71 μM (MCF-7), and 15.23 ± 0.95 μM (4T1).
Showed an IC50 of 28.12 ± 1.49 μM against normal MCF-10a cells, which was significantly higher than against tumor cells.
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Cell Line:Human breast cancer MDA-MB-231 cells
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Concentration:5-20 μM
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Incubation Time:24 h
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Result:Downregulated c-Myc and KRAS protein expression in a dose-dependent manner.
Suppressed the NRF2 signaling pathway, reducing the expression of XCT and GPX4.
Decreased the expression of Caspase 7, Caspase 3, and anti-apoptotic Bcl-2, while increased Cleaved Caspase 3 expression at 20 μM.
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Cell Line:Human breast cancer MDA-MB-231 cells
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Concentration:5-20 μM
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Incubation Time:24 h
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Result:Triggered a dose-dependent increase in both early apoptotic and late apoptotic cell populations.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 4 weeks old, subcutaneously inoculated with 4×105 4T1 mouse breast cancer cells)[1]
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Dosage:10 mg/kg
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Administration:every other day; 14 days
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Result:Reduced final tumor weight.
Suppressed tumor growth.
Elevated percentage of CD45+CD3+CD4+ helper T cells in spleens and in tumors.
Elevated percentage of CD45+CD3+CD8+ cytotoxic T lymphocytes in spleens and in tumors.
Induced downregulation of GPX4 and upregulation of Cleaved Caspase 3 in tumor tissues.
Did not cause significant mouse weight loss or major organ weight changes relative to controls.
Chemical Information
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Masse moléculaire 492.66
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Formule C31H36N6
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SMILES
CN1CCN(CC1)C2=CC=C(C=C2)C3=C(NC(C4=CC=CC=C4)=N3)C5=CC=C(C=C5)N6CCN(CC6)C
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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)
Anticancer agent 309 Related Classifications
Cat. No.: HY-182055
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- Anticancer agent 309
- Anticancer agent309
- Anticancer agent-309
- G-quadruplex
- Keap1-Nrf2
- Ferroptosis
- Apoptosis
- ferroptosis
- parallel G-quadruplexes
- immunogenic cell death
- c-Myc G-quadruplex
- CD4+ helper T lymphocytes
- NRF2-XCT-GPX4 pathway
- apoptosis
- breast cancer cells
- KRAS G-quadruplex
- CD8+ cytotoxic T lymphocytes
- Inhibitor
- inhibitor
- inhibit