Antitumor agent-214
Antitumor agent-214 is a chalcone analogue with anti-tumor activity. Antitumor agent-214 induces cell cycle arrest and apoptosis in tumor cells, disrupts mitochondrial metabolism, and upregulates the expression of caspase 3, caspase 7 and caspase 9, downregulates PARP1. Antitumor agent-214 can be used for anti-tumor research related to colorectal cancer, breast cancer, lung cancer, and cervical cancer.
For research use only. We do not sell to patients.
- CAS No.: 1911631-77-0
- Formula: C19H16N2O4
- Molecular Weight:336.34
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Caspase Isoforms
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Biological Activity
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Caspase 3 |
Caspase-7 |
Caspase-9 |
PARP-1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
12.7 μM
Compound: 3f
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Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTS assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTS assay
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[PMID: 30472605] |
Antitumor agent-214 (Compound 3f) exhibits cytotoxic activity against HCT-116 cells (IC50 = 3.56 μM), MCF-7 cells (IC50 = 4.08 μM), A549 cells (IC50 = 12.70 μM), HeLa cells (IC50 = 8.37 μM), HT-29 cells (IC50 = 6.18 μM) and MD-MBA-231 cells (IC50 = 10.62 μM), with lower cytotoxicity against non-cancerous cells MCF-10AMCF-10A (IC50 = 9.81 μM) [1].
Antitumor agent-214 (1.78-7.12 μM; 24 h) causes a dose-dependent accumulation of HCT-116 cells in the sub-G1 phase, indicating induction of apoptosis[1].
Antitumor agent-214 (3.56 μM, 7.12 μM; 24 h) induces apoptosis in HCT-116 cells as confirmed by Annexin V-FITC/PI dual staining (HY-K1073), with the apoptosis rate equivalent to that induced by Staurosporine (HY-15141), and shows weaker apoptotic effect on MCF-10A cells[1].
Antitumor agent-214 (3.56 μM, 7.12 μM; 24 h) induces apoptosis in HCT-116 cells as demonstrated by AO-EB double staining, with the proportion of orange fluorescent apoptotic cells increasing dose-dependently[1].
Antitumor agent-214 (3.56 μM, 7.12 μM; 24 h) increases mitochondrial superoxide production in HCT-116 cells as detected by MitoSOX Red (HY-D1055) staining[1].
Antitumor agent-214 (7.12 μM; 24 h) induces depolarization of mitochondrial transmembrane potential in HCT-116 cells as shown by JC-1 (HY-15534) staining[1].
Antitumor agent-214 (7.12 μM; 4-12 h) promotes the cleavage of PARP1, caspase 3, caspase 7 and caspase 9 in HCT-116 cells as analyzed by WB, with significant accumulation of cleaved proteins at 12 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116 cells
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Concentration:1.78 μM, 3.56 μM, 7.12 μM
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Incubation Time:24 h
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Result:Induced a significant dose-dependent accumulation of cells in the sub-G1 phase, while had no marked effect on the distribution of cells in G0/G1, S and G2/M phases.
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Cell Line:HCT-116 cells
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Concentration:3.56 μM, 7.12 μM
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Incubation Time:24 h
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Result:Induced apoptosis in a dose-dependent manner, the percentage of apoptotic cells induced by antitumor agent-214 was equivalent to that induced by the positive control staurosporine (STS).
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Cell Line:MCF-10A cells
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Concentration:9.81 μM, 19.62 μM
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Incubation Time:24 h
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Result:Induced apoptosis in a dose-dependent manner, the percentage of apoptotic cells induced by antitumor agent-214 was only 54% of that induced by STS, showing lower apoptosis-inducing potency in normal cells than in cancer cells.
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Cell Line:HCT-116 cells
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Concentration:7.12 μM
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Incubation Time:4 h, 8 h, 12 h
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Result:Time-dependently increased the protein levels of cleaved PARP1, cleaved caspase 3, cleaved caspase 7 and cleaved caspase 9, activating the caspase cascade of the mitochondrial death pathway.
Chemical Information
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CAS No. 1911631-77-0
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Molecular Weight 336.34
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Formula C19H16N2O4
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SMILES
O=C1NC(/C=C/C(C2=CC(OC)=CC=C2OC)=O)=NC3=C1C=CC=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- Antitumor agent-214
- 1911631-77-0
- Antitumor agent214
- Antitumor agent 214
- Caspase
- PARP
- Apoptosis
- Anti-tumor
- disrupts mitochondrial metabolism
- cell cycle arrest and apoptosis
- upregulates the expression of caspase 3
- caspase 7 and caspase 9
- colorectal cancer
- breast cancer
- triple-negative breast cancer (TNBC)
- lung cancer
- cervical carcinoma
- HCT-116 cells
- MCF-7 cells
- A549 cells
- HeLa cells
- HT-29 cells
- MD-MBA-231 cells
- MCF-10A cells
- Inhibitor
- inhibitor
- inhibit