Anticancer agent-364
Anticancer agent-364 is a phenylalanine-derived hydrazone heterocyclic compound that exhibits selective cytotoxicity against NSCLC lung cancer cells. Anticancer agent-364 inhibits VEGF-A, VEGFR-1, and VEGFR-2, increases caspase-3/7, caspase-8, and caspase-9 activity, and induces apoptosis. Anticancer agent-364 can be used for research on non-small cell lung cancer.
For research use only. We do not sell to patients.
- Formula: C22H16BrCl2N3O2
- Molecular Weight:505.19
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
VEGFR1 |
VEGFR2 |
Caspase-3 |
Caspase-7 |
Caspase-8 |
Caspase-9 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
15.60 μM
|
Cytotoxicity against human non-small cell lung cancer A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Cytotoxicity against human non-small cell lung cancer A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
|
42561562 |
| BEAS-2B | IC50 |
1200.00 μM
|
Cytotoxicity against human healthy lung epithelial BEAS-2B cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Cytotoxicity against human healthy lung epithelial BEAS-2B cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
|
42561562 |
| PC-9 | IC50 |
22.49 μM
|
Cytotoxicity against human non-small cell lung cancer PC9 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Cytotoxicity against human non-small cell lung cancer PC9 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
|
42561562 |
In Vitro
Anticancer agent-364 (compound 9d) (15.625-1000 μM; 24-72 h) exhibits IC50 = 15.60 μM against A549 cells, IC50 = 22.49 μM against PC9 cells, and IC50 = 1200.00 μM against BEAS-2B normal lung epithelial cells; the selectivity index SI = 76.92 for A549 and SI = 53.36 for PC9[1].
Anticancer agent-364 (IC20-IC50 values; 24 h) selectively induces apoptosis in A549 lung cancer cells, but does not induce apoptosis in healthy BEAS-2B cells[1].
Anticancer agent-364 (7.5-60 μM; 24 h) significantly reduces intracellular VEGF-A, VEGFR-1, and VEGFR-2 protein levels in A549 cells at intermediate concentrations, but has no significant effect on healthy BEAS-2B cells[1].
Anticancer agent-364 significantly activates caspase-3/7, -8, and -9 in A549 lung cancer cells at concentrations of 7.5 and 10 μM, indicating that it triggers both intrinsic and extrinsic apoptotic pathways[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549, BEAS-2B
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Concentration:7.5, 10, 15 μM (A549)
15, 30, 60 μM (BEAS-2B) -
Incubation Time:24 h
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Result:Reduced intracellular VEGF-A, VEGFR-1, and VEGFR-2 protein levels in A549 cells at intermediate concentrations, but has no significant effect on healthy BEAS-2B cells.
Chemical Information
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Molecular Weight 505.19
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Formula C22H16BrCl2N3O2
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SMILES
BrC1=CC=CC(/C=N/NC(C(C2=CC=CC=C2)NC(C3=C(Cl)C=C(Cl)C=C3)=O)=O)=C1
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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)