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製品番号: HY-182055

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Anticancer agent 309

Anticancer agent 309 (Compound HZ-1) is an anticancer agent and G-quadruplex binder, with K_d 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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

分子式: C₃₁H₃₆N₆
分子量:492.66

保管条件:

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

Anticancer agent 309 構造式

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生物活性

製品説明

体外実験

Anticancer agent 309 binds potently to purified c-Myc G4 and KRAS G4 structures, with K_d 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.

Cell Proliferation Assay^[1]

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
Concentration:

Titrated to determine IC₅₀
Incubation Time:

24 h
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.

Western Blot Analysis^[1]

Cell Line:

Human breast cancer MDA-MB-231 cells
Concentration:

5-20 μM
Incubation Time:

24 h
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.

Apoptosis Analysis^[1]

Cell Line:

Human breast cancer MDA-MB-231 cells
Concentration:

5-20 μM
Incubation Time:

24 h
Result:

Triggered a dose-dependent increase in both early apoptotic and late apoptotic cell populations.

体内実験

Anticancer agent 309 (10 mg/kg; once every other day; for 14 consecutive days) exerts potent antitumor effects on BALB/c mice bearing 4T1 breast cancer cells, while increasing the numbers of CD4⁺and CD8⁺ T cells in the spleen and tumor^[1].

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

Animal Model:

BALB/c (female, 4 weeks old, subcutaneously inoculated with 4×10⁵ 4T1 mouse breast cancer cells)^[1]
Dosage:

10 mg/kg
Administration:

every other day; 14 days
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.

化学情報

分子量 492.66
分子式 C₃₁H₃₆N₆
SMILES

CN1CCN(CC1)C2=CC=C(C=C2)C3=C(NC(C4=CC=CC=C4)=N3)C5=CC=C(C=C5)N6CCN(CC6)C
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Liu XZ, et al. Discovery of small-sized tris-aryl imidazoles as bifunctional ligands for c-Myc and KRAS G-quadruplexes. Bioorg Chem. 2026;173:109656. [Content Brief]

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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.

100 mg

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