Anticancer agent 308
Anticancer agent 308 is an AKT inhibitor with antitumor activity. Anticancer agent 308 reduces total AKT protein levels, thereby inhibiting the pro-survival PI3K/AKT signaling pathway. Anticancer agent 308 induces apoptosis, disrupts mitochondrial membrane potential, promotes ROS accumulation in mitochondria, and induces cell cycle arrest. Anticancer agent 308 inhibits cancer cell migration. Anticancer agent 308 is applicable to research related to breast cancer, lung adenocarcinoma, cervical cancer, prostate cancer, and hepatocellular carcinoma.
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- 화학식: C15H11N3O2
- 분자량:265.27
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Anticancer agent 308 (compound 3s) potently inhibits the viability of MCF-7, MDA-MB-231, MDA-MB-468, A549, HepG2, HeLa and PC-3 cancer cells at low micromolar concentrations, while exerting minimal effects on normal NKE cells (IC50 84.15 μM), resulting in a high selectivity index[1].
Anticancer agent 308 can induce dose-dependent cell death in MDA-MB-231 cells and reduce their colony-forming ability, while exhibiting minimal toxicity to NKE cells[1].
Anticancer agent 308 (0.5-2 μM; 24 h) induces concentration-dependent G2/M cell cycle arrest and increases the accumulation of sub-G0 apoptotic cells in MDA-MB-231 cells; regulates the expression and activation of apoptosis-related proteins and inhibits AKT in MDA-MB-231 cells; induces concentration-dependent accumulation of ROS; induces concentration-dependent cleavage of PARP; induces concentration-dependent mitochondrial depolarization; and inhibits the migration of MDA-MB-231 cells in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231
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Concentration:0.5 μM, 1 μM, 2 μM; 2 μM (co-treated with caspase-3 inhibitor)
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Incubation Time:24 h
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Result:Induced overall apoptosis rates of 58.19% (0.5 μM), 58.35% (1 μM), and 66.8% (2 μM).
Reduced apoptosis to 13.12% when co-treated with 2 μM target reagent and a caspase-3 inhibitor.
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Cell Line:MDA-MB-231
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Concentration:0.5 μM, 1 μM, 2 μM
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Incubation Time:24 h
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Result:Increased the proportion of cells in G2/M phase from 12.86% (control) to 19.39% (0.5 μM), 34.51 % (1 μM), and 50.43% (2 μM).
Decreased G1/S population from 70.66% (control) to 40.23% (0.5 μM), 30.11% (1 μM), and 20.19% (2 μM).
Increased subG0 apoptotic cell population from 1.23% (control) to 10.16 % (0.5 μM), 11.16% (1 μM), and 9.26% (2 μM).
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Cell Line:MDA-MB-231
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Concentration:0.5 μM, 1 μM, 2 μM
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Incubation Time:24 h
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Result:Increased cleaved PARP fluorescence intensity to 2.65-fold (0.5 μM), 3.44-fold (1 μM), and 4.25-fold (2 μM) relative to control (1.00).
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Cell Line:MDA-MB-231
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Concentration:0.5 μM, 1 μM, 2 μM
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Incubation Time:24 h
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Result:Reduced wound closure to 92.3% (0.5 μM), 67.8 % (1 μM), and 41.2% (2 μM) relative to control.
Reduced Transwell migration to 72.7% (0.5 μM), 45.7% (1 μM), and 27.8% (2 μM) relative to control.
Chemical Information
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분자량 265.27
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화학식 C15H11N3O2
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SMILES
NC(C1=C(C2=CC=CC=C2)N=C3C=CC=CN3C1=O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- Anticancer agent 308
- Anticancer agent308
- Anticancer agent-308
- Akt
- Apoptosis
- Reactive Oxygen Species (ROS)
- AKT
- caspase-3
- PI3K/AKT signaling pathway
- apoptosis
- PARP
- mitochondrial membrane potential
- normal kidney epithelial cells
- Bax
- reactive oxygen species (ROS)
- triple-negative breast adenocarcinoma
- Inhibitor
- inhibitor
- inhibit