Anticancer agent 310
Anticancer agent 310 is an antitumor agent. Anticancer agent 310 releases nitric oxide to induce mitochondrial ROS burst, triggers mitochondrial dysfunction and activates the Bax/Bcl-2-Cyt c-Caspase-9/Caspase-3 apoptotic pathway. Anticancer agent 310 also reduces the levels of SHMT2 and MTHFD2, decreases the ratios of NADPH/NADP+ and GSH/GSSG, thereby disrupting redox homeostasis and exacerbating intracellular ROS accumulation. Anticancer agent 310 can be used in research related to gastric 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: C33H36N2O12S
- 分子量:684.71
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
製品説明
体外実験
Anticancer agent 310 (compound A9) (0.016-10 μM; 72 h) potently inhibits the proliferation of various human and murine tumor cell lines in vitro[1].
Anticancer agent 310 (1.6-40 nM; 12-14 days) inhibits the long-term colony-forming ability of HGC27 and AGS gastric cancer cells in a concentration-dependent manner[1].
Anticancer agent 310 (50-100 μM; 2 h) releases nitric oxide in HGC27 and AGS gastric cancer cells[1].
Anticancer agent 310 (2 μM; 12 h) induces mitochondrial ROS burst in HGC27 and AGS gastric cancer cells[1].
Anticancer agent 310 (2 μM) induces mitochondrial membrane potential depolarization in HGC27 and AGS gastric cancer cells, and this effect is reversed by ROS scavenging[1].
Anticancer agent 310 (2 μM; 36 h) induces apoptosis in HGC27 and AGS gastric cancer cells[1].
Anticancer agent 310 (0.5-2 μM; 24 h) activates the Bax/Bcl-2-Cyt c-Caspase-9/Caspase-3 mitochondrial apoptotic pathway in HGC27 and AGS gastric cancer cells in a dose-dependent manner in vitro[1].
Anticancer agent 310 (0.5-2 μM; 24 h) downregulates SHMT2 and MTHFD2, key enzymes in the folate one-carbon metabolic pathway, in HGC27 and AGS gastric cancer cells in a dose-dependent manner by inhibiting the transcription factor ATF4[1].
Anticancer agent 310 (2 μM; 12 h) disrupts redox homeostasis in HGC27 and AGS gastric cancer cells and reduces the ratios of NADPH/NADP+ and GSH/GSSG[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7, HepG2, HCT-116, HGC27, U251, AGS, ES-2, A2780, K562, MEG01, CT26
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Concentration:0.016, 0.08, 0.4, 2, 5, 10 μM
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Incubation Time:72 h
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Result:Exhibited sub-micromolar inhibitory activity across all tested cell lines, with IC50 values as follows: MCF-7: 0.19 μM; HepG2: 0.21 μM; HCT-116: 0.22 μM; HGC27: 0.10 μM; U251: 0.14 μM; AGS: 0.02 μM; ES-2: 0.12 μM; A2780: 0.11 μM; K562: 0.12 μM; MEG01: 0.40 μM; CT26: 0.26 μM.
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Cell Line:HGC27, AGS
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Concentration:2 μM
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Incubation Time:36 h
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Result:Increased total apoptotic cells in HGC27 cells from 10.99% (control) to 83.1%.
Induced a total apoptotic rate of 60.9% in AGS cells.
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Cell Line:HGC27, AGS
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Concentration:0.5, 1, 2 μM
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Incubation Time:24 h
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Result:Upregulated the expression of cytoplasmic cytochrome c, Bax, Cleaved Caspase-9, and Cleaved Caspase-3, and downregulated the expression of mitochondrial cytochrome c and Bcl-2 in a dose-dependent manner in both HGC27 and AGS cells.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NCG mice treated HGC27 tumor fragments[1]
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Dosage:5 mg/kg; 10 mg/kg; 15 mg/kg
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Administration:intratumoral; daily; 14 days
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Result:Reduced tumor weight relative to control at 5 mg/kg dose.
Achieved 95.3% tumor growth inhibition (TGI), with 4 out of 6 mice showing complete tumor regression at 10 mg/kg dose.
Achieved 98.78% TGI, with 5 out of 6 mice showing complete tumor regression at 15 mg/kg dose.
Decreased expression of Ki67, SHMT2, and MTHFD2 in tumor tissues relative to control group at 10 mg/kg and 15 mg/kg doses.
Caused no obvious body weight loss or mortality in any dose group.
化学情報
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分子量 684.71
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分子式 C33H36N2O12S
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SMILES
O=C1OCC2=C1CC[C@@]3(C)[C@@]2([H])C[C@H]4[C@]5(O4)[C@@]36[C@@H](O6)[C@H](O7)[C@@]7(C(O)(C)C)[C@H]5OC(CCCCOC8=NON=C8S(=O)(C9=CC=CC=C9)=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
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Anticancer agent 310 関連分類
HY-182284 関連分類
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Keywords
- Anticancer agent 310
- Anticancer agent310
- Anticancer agent-310
- Reactive Oxygen Species (ROS)
- Apoptosis
- Bcl-2 Family
- Caspase
- SHMT
- Methylenetetrahydrofolate Dehydrogenase (MTHFD)
- Cytochrome P450
- GSH/GSSG
- xenograft mouse models
- SHMT2
- Bax/Bcl-2
- Cyt c
- Caspase-9
- Caspase-3
- apoptotic pathway
- MTHFD2
- folate one-carbon metabolism
- AGS cells
- gastric cancer cells
- redox homeostasis
- NADPH/NADP+
- Inhibitor
- inhibitor
- inhibit