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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: C37H36F3IN4S
- 分子量:752.67
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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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] |
化学情報
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分子量 752.67
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)