Anticancer agent 239
Anticancer agent 239 (Compound 5) is a ligand of hTERT promoter G-quadruplex DNA structures (hTERT G4) (Kd = 1.1 μM), and downregulates hTERT expression. Anticancer agent 239 decreases telomerase activity, shortens telomere length, and induces DNA damage, acute cellular senescence, and apoptosis. Anticancer agent 239 causes mitochondrial dysfunction, disrupts iron metabolism and activates ferroptosis in cancer cells. Anticancer agent 239 inhibits tumor growth in MDA-MB-231 xenograft mouse model.
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- Formule: C37H36F3IN4S
- Masse moléculaire:752.67
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
2.1 μM
Compound: 5
|
Cytotoxicity against telomerase-positive human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against telomerase-positive human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 38987863] |
| HeLa | IC50 |
2.6 μM
Compound: 5
|
Cytotoxicity against telomerase-positive human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against telomerase-positive human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 38987863] |
| HepG2 | IC50 |
2.9 μM
Compound: 5
|
Cytotoxicity against telomerase-positive human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against telomerase-positive human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 38987863] |
| HK-2 | IC50 |
9.4 μM
Compound: 5
|
Cytotoxicity against human HK-2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human HK-2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 38987863] |
| HUVEC | IC50 |
8.7 μM
Compound: 5
|
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 38987863] |
| MDA-MB-231 | IC50 |
0.67 μM
Compound: 5
|
Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of TBHP by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of TBHP by MTT assay
|
[PMID: 38987863] |
| MDA-MB-231 | IC50 |
1 μM
Compound: 5
|
Cytotoxicity against telomerase-positive human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against telomerase-positive human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 38987863] |
| MDA-MB-231 | IC50 |
1.2 μM
Compound: 5
|
Cytotoxicity against human MDA-MB-231 cells without hTERT overexpression assessed as inhibition of cell growth measured after 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells without hTERT overexpression assessed as inhibition of cell growth measured after 48 hrs by MTT assay
|
[PMID: 38987863] |
| MDA-MB-231 | IC50 |
3.3 μM
Compound: 5
|
Cytotoxicity against human MDA-MB-231 cells transfected with hTERT-pcDNA3.1(+)-C-eBFP overexpressing hTERT assessed as inhibition of cell growth measured after 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells transfected with hTERT-pcDNA3.1(+)-C-eBFP overexpressing hTERT assessed as inhibition of cell growth measured after 48 hrs by MTT assay
|
[PMID: 38987863] |
| PC-3 | IC50 |
2.5 μM
Compound: 5
|
Cytotoxicity against telomerase-positive human PC-3 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against telomerase-positive human PC-3 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 38987863] |
| U2OS | IC50 |
3.9 μM
Compound: 5
|
Cytotoxicity against alternative lengthening of telomere-positive human U2OS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against alternative lengthening of telomere-positive human U2OS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
|
[PMID: 38987863] |
Chemical Information
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Masse moléculaire 752.67
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Formule C37H36F3IN4S
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SMILES
C[N+]1=C(C=C(C2=CC=CC=C21)/C=C3SC4=C(N\3CCCN5CCC(CC5)C(F)(F)F)C=CC=C4)/C=C/C6=CNC7=C6C=CC=C7.[I-]
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)